WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H333094
CAS#: 1637741-58-2
Description: Ciprofol, also known as HSK3486, is a positive allosteric regulator and direct agonist of GABAA receptor. It has a promising sedative/hypnotic effect and good in vivo pharmacokinetic properties, which justify further studies towards its clinical application.
Hodoodo Cat#: H333094
Name: Ciprofol
CAS#: 1637741-58-2
Chemical Formula: C14H20O
Exact Mass: 204.15
Molecular Weight: 204.313
Elemental Analysis: C, 82.30; H, 9.87; O, 7.83
This product is not in stock, which may be available by custom synthesis.
For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge).
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Synonym: Ciprofol; HSK3486; HSK-3486; HSK 3486;
IUPAC/Chemical Name: Phenol, 2-[(1R)-1-cyclopropylethyl]-6-(1-methylethyl)-
InChi Key: BMEARIQHWSVDBS-SNVBAGLBSA-N
InChi Code: InChI=1S/C14H20O/c1-9(2)12-5-4-6-13(14(12)15)10(3)11-7-8-11/h4-6,9-11,15H,7-8H2,1-3H3/t10-/m1/s1
SMILES Code: OC1=C(C(C)C)C=CC=C1[C@@H](C2CC2)C
Appearance: To be determined
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 204.31 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Wang YC, Wu MJ, Zhou SL, Li ZH. Protective effects of combined treatment with ciprofol and mild therapeutic hypothermia during cerebral ischemia-reperfusion injury. World J Clin Cases. 2023 Jan 26;11(3):487-492. doi: 10.12998/wjcc.v11.i3.487. PMID: 36793629; PMCID: PMC9923870.
2: Liang P, Dai M, Wang X, Wang D, Yang M, Lin X, Zou X, Jiang K, Li Y, Wang L, Shangguan W, Ren J, He H. Efficacy and safety of HSK3486 vs. propofol for the induction and maintenance of general anaesthesia: A multicentre, single-blind, randomised, parallel-group, phase 3 clinical trial. Eur J Anaesthesiol. 2023 Jan 20. doi: 10.1097/EJA.0000000000001799. Epub ahead of print. PMID: 36647565.
3: Yang Y, Xia Z, Xu C, Zhai C, Yu X, Li S. Ciprofol attenuates the isoproterenol-induced oxidative damage, inflammatory response and cardiomyocyte apoptosis. Front Pharmacol. 2022 Nov 22;13:1037151. doi: 10.3389/fphar.2022.1037151. PMID: 36483733; PMCID: PMC9723392.
4: Hu Y, Li X, Liu J, Chen H, Zheng W, Zhang H, Wu M, Li C, Zhu X, Lou J, Yan P, Wu N, Liu X, Ma S, Wang X, Ding Y, Xuan C. Safety, pharmacokinetics and pharmacodynamics of a novel γ-aminobutyric acid (GABA) receptor potentiator, HSK3486, in Chinese patients with hepatic impairment. Ann Med. 2022 Dec;54(1):2769-2780. doi: 10.1080/07853890.2022.2129433. PMID: 36217101; PMCID: PMC9559057.
5: Li J, Wang X, Liu J, Wang X, Li X, Wang Y, Ouyang W, Li J, Yao S, Zhu Z, Guo Q, Yu Y, Meng J, Zuo Y. 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 Clin Pharmacol Toxicol. 2022 Aug;131(2):138-148. doi: 10.1111/bcpt.13761. Epub 2022 Jun 10. PMID: 35653554; PMCID: PMC9543620.
6: Zeng Y, Wang DX, Lin ZM, Liu J, Wei XC, Deng J, Liu YF, Ma EL, Yang MC, Zheng H, Yu XD, Guo QL, Guan YJ. 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. Eur Rev Med Pharmacol Sci. 2022 Feb;26(4):1114-1124. doi: 10.26355/eurrev_202202_28101. PMID: 35253166.
7: Liao J, Li M, Huang C, Yu Y, Chen Y, Gan J, Xiao J, Xiang G, Ding X, Jiang R, Li P, Yang M. Pharmacodynamics and Pharmacokinetics of HSK3486, a Novel 2,6-Disubstituted Phenol Derivative as a General Anesthetic. Front Pharmacol. 2022 Feb 3;13:830791. doi: 10.3389/fphar.2022.830791. PMID: 35185584; PMCID: PMC8851058.
8: Luo Z, Tu H, Zhang X, Wang X, Ouyang W, Wei X, Zou X, Zhu Z, Li Y, Shangguan W, Wu H, Wang Y, Guo Q. 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. 2022 Mar;36(3):301-313. doi: 10.1007/s40263-021-00890-1. Epub 2022 Feb 14. PMID: 35157236; PMCID: PMC8927014.
9: Liu Y, Yu X, Zhu D, Zeng J, Lin Q, Zang B, Chen C, Liu N, Liu X, Gao W, Guan X. 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. Chin Med J (Engl). 2022 May 5;135(9):1043-1051. doi: 10.1097/CM9.0000000000001912. PMID: 34924506; PMCID: PMC9276409.
10: Li X, Yang D, Li Q, Wang H, Wang M, Yan P, Wu N, Li F, Ma S, Ding Y, Liu J, Wang H. Safety, Pharmacokinetics, and Pharmacodynamics of a Single Bolus of the γ-aminobutyric Acid (GABA) Receptor Potentiator HSK3486 in Healthy Chinese Elderly and Non-elderly. Front Pharmacol. 2021 Aug 27;12:735700. doi: 10.3389/fphar.2021.735700. PMID: 34512361; PMCID: PMC8430033.
11: Assessments of Onset and Duration of Drug Effects and Pharmacokinetics by Dose Level of HSK3486, a New Sedative-Hypnotic Agent, in Healthy Female/Male Subjects: A Phase I Multiarm Randomized Controlled Clinical Trial: Retraction. Anesth Analg. 2021 Jul 1;133(1):e16. doi: 10.1213/ANE.0000000000005570. PMID: 34127606; PMCID: PMC8253502.
12: Ludbrook G, Li F, Sleigh J, Liang Y. Assessments of Onset and Duration of Drug Effects and Pharmacokinetics by Dose Level of HSK3486, a New Sedative- Hypnotic Agent, in Healthy Female/Male Subjects: A Phase I Multiarm Randomized Controlled Clinical Trial [Retracted]. Anesth Analg. 2021 Jan 15. doi: 10.1213/ANE.0000000000005343. Epub ahead of print. Retraction in: Anesth Analg. 2021 Jul 1;133(1):e16. PMID: 33464758.
13: Bian Y, Zhang H, Ma S, Jiao Y, Yan P, Liu X, Ma S, Xiong Y, Gu Z, Yu Z, Huang C, Miao L. Mass balance, pharmacokinetics and pharmacodynamics of intravenous HSK3486, a novel anaesthetic, administered to healthy subjects. Br J Clin Pharmacol. 2021 Jan;87(1):93-105. doi: 10.1111/bcp.14363. Epub 2020 Aug 3. PMID: 32415708.
14: Wei Y, Qiu G, Lei B, Qin L, Chu H, Lu Y, Zhu G, Gao Q, Huang Q, Qian G, Liao P, Luo X, Zhang X, Zhang C, Li Y, Zheng S, Yu Y, Tang P, Ni J, Yan P, Zhou Y, Li P, Huang X, Gong A, Liu J. Oral Delivery of Propofol with Methoxymethylphosphonic Acid as the Delivery Vehicle. J Med Chem. 2017 Oct 26;60(20):8580-8590. doi: 10.1021/acs.jmedchem.7b01133. Epub 2017 Oct 12. PMID: 28968087.
15: Qin L, Ren L, Wan S, Liu G, Luo X, Liu Z, Li F, Yu Y, Liu J, Wei Y. Design, Synthesis, and Evaluation of Novel 2,6-Disubstituted Phenol Derivatives as General Anesthetics. J Med Chem. 2017 May 11;60(9):3606-3617. doi: 10.1021/acs.jmedchem.7b00254. Epub 2017 Apr 28. PMID: 28430430.
