Cipepofol

It's only fair to share...Flattr the authorPin on PinterestEmail this to someone
Buffer this pageDigg thisShare on FacebookShare on Google+Tweet about this on TwitterShare on LinkedInShare on YummlyShare on VKShare on RedditShare on StumbleUponPrint this pageShare on Tumblr

Cipepofol

CAS1637741-58-2

MW 204.31 g/mol MF C14H20O

2-[(1R)-1-cyclopropylethyl]-6-propan-2-ylphenol

FDA 2026, APPROVALS 2026, Cypsedo, HSK 3486, CS-0064163, GTPL 10812, HSK-3486, HY-116152, M3WGS532VY

  • OriginatorSichuan Haisco Pharmaceutical
  • ClassCyclopropanes; General anaesthetics; Phenols; Small molecules
  • Mechanism of ActionGABA A receptor agonists
  • RegisteredAnaesthesia; Sedation
  • 10 Apr 2026Sichuan Haisco Pharmaceutical plans a phase III trial for Anesthesia (In Children, In adolescents) (IV) in May 2026 (NCT07510945)
  • 28 Aug 2024No recent reports of development identified for preclinical development in Sedation in USA (IV, Infusion)
  • 01 Aug 2024Zhongda Hospital plans a clinical trial for Sedation (IV) in August 2024 (NCT06538883)

To induce general anesthesia in adults undergoing surgery

Cipepofol (also known as ciprofol or HSK3486) is a novel, short-acting intravenous anesthetic and sedative. As a structural analog of propofol, it targets \(GABA_{A}\) receptors but is 4 to 6 times more potent. It offers faster recovery, improved cardiovascular stability, and significantly less injection pain than propofol.

Key Clinical Advantages

  • Superior Efficacy: Requires a lower dose to achieve the same sedative depth as propofol.
  • Better Safety Profile: Associated with a lower incidence of injection pain, reduced respiratory depression, and better hemodynamic (blood pressure) stability.
  • Fast Acting: Characterized by rapid onset and quick recovery times, making it ideal for procedures like gastrointestinal endoscopy, bronchoscopy, and general anesthesia induction.

Recent Developments

  • FDA Approval: Cipepofol (sold under the brand name CYPSEDO) officially received U.S. FDA marketing approval, becoming the first China-originated innovative intravenous anesthetic to enter the global market.
  • Ongoing Trials: Clinical trials and post-marketing studies are actively evaluating its safety in specific populations, such as elderly patients and children.

Cipepofol (INNTooltip International Nonproprietary Name, USANTooltip United States Adopted Name), also known as ciprofol or by its developmental code name HSK3486, is a general anesthetic related to propofol which is used for anesthesia and sedation.[1][2][3][4] The drug is used by intravenous infusion.[1] A short-acting and highly selective γ-aminobutyric acid positive allosteric modulator,[5] ciprofol is 4 to 6 times more potent than other phenol derivatives such as propofol or fospropofol.[6]

In May 2026, cipepofol was approved by the US FDA.[7] Manufactured by Haisco Pharmaceutical Group of Chengdu, Sichuan, China, ciprofol underwentphase I and II trials in Australia and China.[8][9][10] In these early studies, ciprofol was comparable in efficacy to propofol and was associated with fewer adverse events.[4][6][11][12][13][14][15][16][17][18]

Physical properties

Ciprofol is an optically active 2,6-disubstituted alkylphenol with a cyclopropylethyl group incorporated at the second carbon atom. This cyclopropyl group increases the steric effects and introduces stereoselective effects over its anesthetic properties. These properties appear to increase the anesthetic potency of ciprofol, when compared with propofol.[9]

Medical use

Ciprofol is used for the intravenous induction of general anesthesia.[3][4] Studies published in 2022 and 2023 found it was efficacious as a general anesthetic in patients undergoing gynecological surgery[6][11] and kidney transplantation,[19] as well as for endoscopic procedures such as bronchoscopy,[15][20] esophagogastroduodenoscopy and colonoscopy.[21][22]

Ciprofol has also been used for sedation of critically ill patients undergoing mechanical ventilation in the intensive care unit,[23] as well as for the treatment of agitation and delirium in that patient population.[24] When combined with mild therapeutic hypothermia, ciprofol may also be useful as a cerebral protective agent in the setting of cerebral ischemia-reperfusion injury.[25]

Experimental use

In experimental models of isoproterenol-induced myocardial infarction (using mice as subjects), ciprofol appears to protect the heart against oxidative damage, inflammation and apoptosis of cardiac muscle cells.[26]

SYN

US20240132445,

https://patentscope.wipo.int/search/en/detail.jsf?docId=US428011434&_cid=P12-MPW0XO-91017-1

PAT

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2014180305&_cid=P12-MPW0R4-87054-1

Example 16

[-cyclopropylethyl] -6 -isopropylphenol (compound 16)

2- [(lR)-l-cyclopropylethyl]-6-isopropyl -phenol

Preparation methods of Examples 16-17:

2-(1-Cyclopropylethyl-6-isopropylphenol (compound 3) 600 mg was used for resolution. Preparation conditions: (Instrument: Agilent 1260/CH-Y-J0404; Column: CHIRALPAK OJ-H (4.6 mm < 250 mm, 5 μm) No.: OJ-H-27; Mobile phase: A: isopropanol, B: n-hexane; Flow rate: 1.0 mL/min; Back pressure: 100 bar; Column temperature: 35°C; Wavelength: 210 nm; Period: 10 min)

Two optical isomers were obtained after separation: peak 1 (retention time: 10.72 min, 280 mg, pale yellow liquid, ee%=99%) and peak 2 (retention time: 13.58 min, 280 mg, pale yellow liquid, ee%=99%).

峰 1 : MS m/z(ESI): 203.1(Ml).

toMR (400 MHz,CDCl3 ) ： δ 7.14(dd， 1H)， δ 7.08(dd， 1H)， 6.91 (t， 1H)， 4.93 (s, 1H), 3.22-3.14(m, 1H)， 2.55-2.48 (m, 1H)， 1.33 (d, 6H)， 1.28 (d, 3H)， 1.10-1.05 (m， 1H)， 0.60-0.58 (m, 1H)， 0.49-0.46 (m， 1H)， 0.25-0.18 (m, 2H).

峰 2: MS m/z(ESI): 203.1(Ml).

iHNMR (400 MHz,CDCl3) ： 57.14(dd, 1H)， δ 7.08(dd， 1H)， 6.93 (t, 1H)， 4.93 (s 1H), 3.22-3.15(m, 1H)， 2.55-2.48 (m， 1H)， 1.32 (d， 6H)， 1.28 (d， 3H)， 1.10-1.04 (m， 1H)， 0.60-0.58 (m, 1H)， 0.49-0.46 (m, 1H)， 0.25-0.18 (m, 2H).

PAT

ADVERTISEMENT

ANAX LABORATORIES

WEBSITE https://www.anaxlab.com/

Discovery Solutions, Supporting the chemistry needs of clients in the Medical, Analytical and Bio Sciences

Development Solutions, Developing from Lab scale to PR&D, Kilo Scale-ups and Commercial Scales

SEE MORE………Integrated Solutions, Manufacturing Solutions, Products,
Can’t Find? Let’s Connect

Phone : +91 897704 2010 /  +91 9177075735, Email : info@anaxlab.com

#MedicinalChemistry, #DrugDiscovery, #OrganicSynthesis, #ChemicalLibrary, #BuildingBlocks, #SARStudies, #ChemistryInnovation, #medchem, #Drugdevelopment, #Biotech, #Biotechnology, #AnaxLaboratories, #Pharma

str1

AS ON FEB2026 4.574 LAKHS VIEWS ON BLOG WORLDREACH AVAILABLEFOR YOUR ADVERTISEMENT

wdt-16

join me on Linkedin

Anthony Melvin Crasto Ph.D – India | LinkedIn

join me on Researchgate

RESEARCHGATE

This image has an empty alt attribute; its file name is research.jpg

join me on Facebook

Anthony Melvin Crasto Dr. | Facebook

join me on twitter

Anthony Melvin Crasto Dr. | twitter

+919321316780 call whatsaapp

EMAIL. amcrasto@gmail.com

References

References

  1.  “Sichuan Haisco Pharmaceutical”. AdisInsight. 28 August 2024. Retrieved 1 October 2025.
  2.  “Ciprofol (Cipepofol): A γ-Aminobutyric Acid Receptor Agonist for Induction of Anesthesia”. Chemistry and Pharmacology of Drug Discovery. Wiley. 2024. pp. 251–274. doi:10.1002/9781394225156.ch12. ISBN 978-1-394-22512-5. Retrieved 1 October 2025.
  3.  Wang X, Wang X, Liu J, Zuo YX, Zhu QM, Wei XC, et al. (March 2022). “Effects of ciprofol for the induction of general anesthesia in patients scheduled for elective surgery compared to propofol: a phase 3, multicenter, randomized, double-blind, comparative study”. European Review for Medical and Pharmacological Sciences. 26 (5): 1607–1617. PMID 35302207.
  4.  Zeng Y, Wang DX, Lin ZM, Liu J, Wei XC, Deng J, et al. (February 2022). “Efficacy and safety of HSK3486 for the induction and maintenance of general anesthesia in elective surgical patients: a multicenter, randomized, open-label, propofol-controlled phase 2 clinical trial”. European Review for Medical and Pharmacological Sciences. 26 (4): 1114–1124. PMID 35253166.
  5.  Liao J, Li M, Huang C, Yu Y, Chen Y, Gan J, et al. (2022). “Pharmacodynamics and Pharmacokinetics of HSK3486, a Novel 2,6-Disubstituted Phenol Derivative as a General Anesthetic”. Frontiers in Pharmacology. 13 830791. doi:10.3389/fphar.2022.830791. PMC 8851058. PMID 35185584.
  6.  Chen BZ, Yin XY, Jiang LH, Liu JH, Shi YY, Yuan BY (August 2022). “The efficacy and safety of ciprofol use for the induction of general anesthesia in patients undergoing gynecological surgery: a prospective randomized controlled study”. BMC Anesthesiology. 22 (1) 245. doi:10.1186/s12871-022-01782-7. PMC 9347095. PMID 35922771.
  7.  “Novel Drug Approvals for 2026”. U.S. Food and Drug Administration. 29 May 2026. Retrieved 31 May 2026.
  8.  Lu M, Liu J, Wu X, Zhang Z (2023). “Ciprofol: A Novel Alternative to Propofol in Clinical Intravenous Anesthesia?”. BioMed Research International. 2023 7443226. doi:10.1155/2023/7443226. PMC 9879693. PMID 36714027.
  9.  Qin L, Ren L, Wan S, Liu G, Luo X, Liu Z, et al. (May 2017). “Design, Synthesis, and Evaluation of Novel 2,6-Disubstituted Phenol Derivatives as General Anesthetics”. Journal of Medicinal Chemistry. 60 (9): 3606–3617. doi:10.1021/acs.jmedchem.7b00254. PMID 28430430.
  10.  Nair A, Seelam S (2022). “Ciprofol- a game changing intravenous anesthetic or another experimental drug!”. Saudi Journal of Anaesthesia. 16 (2): 258–259. doi:10.4103/sja.sja_898_21. PMC 9009555. PMID 35431734.
  11.  Man Y, Xiao H, Zhu T, Ji F (March 2023). “Study on the effectiveness and safety of ciprofol in anesthesia in gynecological day surgery: a randomized double-blind controlled study”. BMC Anesthesiology. 23 (1) 92. doi:10.1186/s12871-023-02051-x. PMC 10039513. PMID 36964501.
  12.  Chen X, Guo P, Yang L, Liu Z, Yu D (2022). “Comparison and Clinical Value of Ciprofol and Propofol in Intraoperative Adverse Reactions, Operation, Resuscitation, and Satisfaction of Patients under Painless Gastroenteroscopy Anesthesia”. Contrast Media & Molecular Imaging. 2022 9541060. doi:10.1155/2022/9541060. PMC 9314164. PMID 35935320.
  13.  Zhong J, Zhang J, Fan Y, Zhu M, Zhao X, Zuo Z, et al. (May 2023). “Efficacy and safety of Ciprofol for procedural sedation and anesthesia in non-operating room settings”. Journal of Clinical Anesthesia. 85 111047. doi:10.1016/j.jclinane.2022.111047. PMID 36599219. S2CID 255468218.
  14.  Liang P, Dai M, Wang X, Wang D, Yang M, Lin X, et al. (June 2023). “Efficacy and safety of ciprofol vs. propofol for the induction and maintenance of general anaesthesia: A multicentre, single-blind, randomised, parallel-group, phase 3 clinical trial”. European Journal of Anaesthesiology. 40 (6): 399–406. doi:10.1097/EJA.0000000000001799. PMC 10155686. PMID 36647565.
  15.  Luo Z, Tu H, Zhang X, Wang X, Ouyang W, Wei X, et al. (March 2022). “Efficacy and Safety of HSK3486 for Anesthesia/Sedation in Patients Undergoing Fiberoptic Bronchoscopy: A Multicenter, Double-Blind, Propofol-Controlled, Randomized, Phase 3 Study”. CNS Drugs. 36 (3): 301–313. doi:10.1007/s40263-021-00890-1. PMC 8927014. PMID 35157236.
  16.  Hu C, Ou X, Teng Y, Shu S, Wang Y, Zhu X, et al. (November 2021). “Sedation Effects Produced by a Ciprofol Initial Infusion or Bolus Dose Followed by Continuous Maintenance Infusion in Healthy Subjects: A Phase 1 Trial”. Advances in Therapy. 38 (11): 5484–5500. doi:10.1007/s12325-021-01914-4. PMC 8523013. PMID 34559359.
  17.  Teng Y, Ou M, Wang X, Zhang W, Liu X, Liang Y, et al. (September 2021). “Efficacy and safety of ciprofol for the sedation/anesthesia in patients undergoing colonoscopy: Phase IIa and IIb multi-center clinical trials”. European Journal of Pharmaceutical Sciences. 164 105904. doi:10.1016/j.ejps.2021.105904. PMID 34116176.
  18.  Zhu Q, Luo Z, Wang X, Wang D, Li J, Wei X, et al. (April 2023). “Efficacy and safety of ciprofol versus propofol for the induction of anesthesia in adult patients: a multicenter phase 2a clinical trial”. International Journal of Clinical Pharmacy. 45 (2): 473–482. doi:10.1007/s11096-022-01529-x. PMC 10147789. PMID 36680620.
  19.  Qin K, Qin WY, Ming SP, Ma XF, Du XK (July 2022). “Effect of ciprofol on induction and maintenance of general anesthesia in patients undergoing kidney transplantation”. European Review for Medical and Pharmacological Sciences. 26 (14): 5063–5071. PMID 35916802.
  20.  Wu B, Zhu W, Wang Q, Ren C, Wang L, Xie G (2022). “Efficacy and safety of ciprofol-remifentanil versus propofol-remifentanil during fiberoptic bronchoscopy: A prospective, randomized, double-blind, non-inferiority trial”. Frontiers in Pharmacology. 13 1091579. doi:10.3389/fphar.2022.1091579. PMC 9812563. PMID 36618929.
  21.  Li J, Wang X, Liu J, Wang X, Li X, Wang Y, et al. (August 2022). “Comparison of ciprofol (HSK3486) versus propofol for the induction of deep sedation during gastroscopy and colonoscopy procedures: A multi-centre, non-inferiority, randomized, controlled phase 3 clinical trial”. Basic & Clinical Pharmacology & Toxicology. 131 (2): 138–148. doi:10.1111/bcpt.13761. PMC 9543620. PMID 35653554.
  22.  Long YQ, Feng CD, Ding YY, Feng XM, Liu H, Ji FH, et al. (2022). “Esketamine as an Adjuvant to Ciprofol or Propofol Sedation for Same-Day Bidirectional Endoscopy: Protocol for a Randomized, Double-Blind, Controlled Trial With Factorial Design”. Frontiers in Pharmacology. 13 821691. doi:10.3389/fphar.2022.821691. PMC 8975265. PMID 35370640.
  23.  Liu Y, Yu X, Zhu D, Zeng J, Lin Q, Zang B, et al. (May 2022). “Safety and efficacy of ciprofol vs. propofol for sedation in intensive care unit patients with mechanical ventilation: a multi-center, open label, randomized, phase 2 trial”. Chinese Medical Journal. 135 (9): 1043–1051. doi:10.1097/CM9.0000000000001912. PMC 9276409. PMID 34924506.
  24.  Liu GL, Wu GZ, Ge D, Zhou HJ, Cui S, Gao K, et al. (2023). “Efficacy and safety of ciprofol for agitation and delirium in the ICU: A multicenter, single-blind, 3-arm parallel randomized controlled trial study protocol”. Frontiers in Medicine. 9 1024762. doi:10.3389/fmed.2022.1024762. PMC 9868613. PMID 36698817.
  25.  Wang YC, Wu MJ, Zhou SL, Li ZH (January 2023). “Protective effects of combined treatment with ciprofol and mild therapeutic hypothermia during cerebral ischemia-reperfusion injury”. World Journal of Clinical Cases. 11 (3): 487–492. doi:10.12998/wjcc.v11.i3.487. PMC 9923870. PMID 36793629.
  26.  Yang Y, Xia Z, Xu C, Zhai C, Yu X, Li S (2022). “Ciprofol attenuates the isoproterenol-induced oxidative damage, inflammatory response and cardiomyocyte apoptosis”. Frontiers in Pharmacology. 13 1037151. doi:10.3389/fphar.2022.1037151. PMC 9723392. PMID 36483733.
  27.  Vittori A, Di Fabio C, Cascella M, Marinangeli F, Francia E, Mascilini I, et al. (January 2026). “Advantages of Ciprofol with Special Consideration of Pediatric Anesthesia”. Children (Basel, Switzerland). 13 (2). doi:10.3390/children13020188. PMC 12939459. PMID 41749542.
  28.  Liu SB, Yao X, Tao J, Yang JJ, Zhao YY, Liu DW, et al. (March 2023). “Population total and unbound pharmacokinetics and pharmacodynamics of ciprofol and M4 in subjects with various renal functions”. British Journal of Clinical Pharmacology. 89 (3): 1139–1151. doi:10.1111/bcp.15561. PMID 36217805. S2CID 252818288.
  29.  Hu Y, Li X, Liu J, Chen H, Zheng W, Zhang H, et al. (December 2022). “Safety, pharmacokinetics and pharmacodynamics of a novel γ-aminobutyric acid (GABA) receptor potentiator, HSK3486, in Chinese patients with hepatic impairment”. Annals of Medicine. 54 (1): 2769–2780. doi:10.1080/07853890.2022.2129433. PMC 9559057. PMID 36217101.
  30.  Li X, Yang D, Li Q, Wang H, Wang M, Yan P, et al. (2021). “Safety, Pharmacokinetics, and Pharmacodynamics of a Single Bolus of the γ-aminobutyric Acid (GABA) Receptor Potentiator HSK3486 in Healthy Chinese Elderly and Non-elderly”. Frontiers in Pharmacology. 12 735700. doi:10.3389/fphar.2021.735700. PMC 8430033. PMID 34512361.
  31.  Ding YY, Long YQ, Yang HT, Zhuang K, Ji FH, Peng K (December 2022). “Efficacy and safety of ciprofol for general anaesthesia induction in elderly patients undergoing major noncardiac surgery: A randomised controlled pilot trial”. European Journal of Anaesthesiology. 39 (12): 960–963. doi:10.1097/EJA.0000000000001759. PMID 36214498. S2CID 252779399.
  32.  Duan G, Lan H, Shan W, Wu Y, Xu Q, Dong X, et al. (April 2023). “Clinical effect of different doses of ciprofol for induction of general anesthesia in elderly patients: A randomized, controlled trial”. Pharmacology Research & Perspectives. 11 (2) e01066. doi:10.1002/prp2.1066. PMC 9944862. PMID 36811327. S2CID 257098376.
  33.  Yang Y, Xia Z, Xu C, Zhai C, Yu X, Li S (2022). “Ciprofol attenuates the isoproterenol-induced oxidative damage, inflammatory response and cardiomyocyte apoptosis”. Frontiers in Pharmacology. 13 1037151: 1037151. doi:10.3389/fphar.2022.1037151. PMC 9723392. PMID 36483733.
  34.  Bian Y, Zhang H, Ma S, Jiao Y, Yan P, Liu X, et al. (January 2021). “Mass balance, pharmacokinetics and pharmacodynamics of intravenous HSK3486, a novel anaesthetic, administered to healthy subjects”. British Journal of Clinical Pharmacology. 87 (1): 93–105. doi:10.1111/bcp.14363. PMID 32415708. S2CID 218658207.

Further reading

Clinical data
Other namesCiprofol; CS-0064163; CS0064163; GTPL10812; GTPL-10812; HSK-3486; HSK3486; HY-116152; HY116152; (R)-2-(1-Cyclopropylethyl)-6-isopropylphenol
Routes of
administration		Intravenous infusion[1]
Drug classGABAA receptor positive allosteric modulator
Pharmacokinetic data
MetabolismLiver glucuronidation
ExcretionKidney
Identifiers
IUPAC name
CAS Number1637741-58-2 
PubChem CID86301664
DrugBankDB16295 
ChemSpider76794458 
UNIIM3WGS532VY
KEGGD12449 
ChEMBLChEMBL4094894 
Chemical and physical data
FormulaC14H20O
Molar mass204.313 g·mol−1
3D model (JSmol)Interactive image
SMILES
InChI

////////cipepofol, FDA 2026, APPROVALS 2026, Cypsedo, HSK 3486, CS-0064163, GTPL 10812, HSK-3486, HY-116152, M3WGS532VY, ANAESTHETIC

It's only fair to share...Flattr the authorPin on PinterestEmail this to someone
Buffer this pageDigg thisShare on FacebookShare on Google+Tweet about this on TwitterShare on LinkedInShare on YummlyShare on VKShare on RedditShare on StumbleUponPrint this pageShare on Tumblr

Leave a Reply

Your email address will not be published. Required fields are marked *

➤