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MedKoo Cat#: 591166 | Name: Drofenine hydrochloride
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Drofenine hydrochloride is a widely used anticholinergic drug. It acts on smooth muscle to inhibit muscle spasms.

Chemical Structure

Drofenine hydrochloride
Drofenine hydrochloride
CAS#548-66-3 (HCl)

Theoretical Analysis

MedKoo Cat#: 591166

Name: Drofenine hydrochloride

CAS#: 548-66-3 (HCl)

Chemical Formula: C20H32ClNO2

Exact Mass: 0.0000

Molecular Weight: 353.93

Elemental Analysis: C, 67.87; H, 9.11; Cl, 10.02; N, 3.96; O, 9.04

Price and Availability

Size Price Availability Quantity
50mg USD 350.00 2 Weeks
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Related CAS #
1679-76-1 (free base) 548-66-3 (HCl)
Synonym
Cycloadiphenine hydrochloride; Cycloadiphenine HCl; Cyclovegantine; Hexahydroadiphenine;
IUPAC/Chemical Name
2-(diethylamino)ethyl 2-cyclohexyl-2-phenylacetate hydrochloride
InChi Key
WIELVDXKOYPANK-UHFFFAOYSA-N
InChi Code
InChI=1S/C20H31NO2.ClH/c1-3-21(4-2)15-16-23-20(22)19(17-11-7-5-8-12-17)18-13-9-6-10-14-18;/h5,7-8,11-12,18-19H,3-4,6,9-10,13-16H2,1-2H3;1H
SMILES Code
O=C(OCCN(CC)CC)C(C1CCCCC1)C2=CC=CC=C2.[H]Cl
Appearance
Solid powder
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
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
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
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Drofenine hydrochloride is a potent competitive inhibitor of BChE, and the ki values of Drofenine is calculated to be 3 uM.
In vitro activity:
Drofenine exhibited similar potency to the known TRPV3 agonists 2-aminoethoxydiphenylboronate (2-APB) and carvacrol in HEK-293 cells, but greater selectivity for TRPV3 based on a lack of activation of TRPA1, V1, V2, V4, or M8. Reference: Pharmacol Res Perspect. 2014 Oct;2(5):e00062. https://pubmed.ncbi.nlm.nih.gov/25089200/
In vivo activity:
This study reports that antispasmodic drug drofenine (Dfe) blocks Kv2.1 and ameliorates DPN-like pathology in diabetic mice. The underlying mechanisms are investigated against the DPN mice with in vivo Kv2.1 knockdown through adeno associated virus AAV9-Kv2.1-RNAi. Streptozotocin (STZ) induced type 1 or db/db type 2 diabetic mice with DPN exhibited a high level of Kv2.1 protein in dorsal root ganglion (DRG) tissue and a suppressed neurite outgrowth in DRG neuron. Reference: iScience. 2020 Sep 28;23(10):101617. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7559245/
Solvent mg/mL mM
Solubility
Water 33.3 94.09
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 353.93 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.

Recalculate based on batch purity %
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:
1. Deering-Rice CE, Mitchell VK, Romero EG, Abdel Aziz MH, Ryskamp DA, Križaj D, Gopal VR, Reilly CA. Drofenine: A 2-APB Analogue with Greater Selectivity for Human TRPV3. Pharmacol Res Perspect. 2014 Oct;2(5):e00062. doi: 10.1002/prp2.62. PMID: 25089200; PMCID: PMC4115637. 2. Xu X, Xu X, Hao Y, Zhu X, Lu J, Ouyang X, Lu Y, Huang X, Li Y, Wang J, Shen X. Antispasmodic Drug Drofenine as an Inhibitor of Kv2.1 Channel Ameliorates Peripheral Neuropathy in Diabetic Mice. iScience. 2020 Sep 28;23(10):101617. doi: 10.1016/j.isci.2020.101617. PMID: 33089105; PMCID: PMC7559245.
In vitro protocol:
1. Deering-Rice CE, Mitchell VK, Romero EG, Abdel Aziz MH, Ryskamp DA, Križaj D, Gopal VR, Reilly CA. Drofenine: A 2-APB Analogue with Greater Selectivity for Human TRPV3. Pharmacol Res Perspect. 2014 Oct;2(5):e00062. doi: 10.1002/prp2.62. PMID: 25089200; PMCID: PMC4115637.
In vivo protocol:
1. Xu X, Xu X, Hao Y, Zhu X, Lu J, Ouyang X, Lu Y, Huang X, Li Y, Wang J, Shen X. Antispasmodic Drug Drofenine as an Inhibitor of Kv2.1 Channel Ameliorates Peripheral Neuropathy in Diabetic Mice. iScience. 2020 Sep 28;23(10):101617. doi: 10.1016/j.isci.2020.101617. PMID: 33089105; PMCID: PMC7559245.
1: Deering-Rice CE, Mitchell VK, Romero EG, Abdel Aziz MH, Ryskamp DA, Križaj D, Gopal VR, Reilly CA. Drofenine: A 2-APB Analogue with Greater Selectivity for Human TRPV3. Pharmacol Res Perspect. 2014 Oct;2(5):e00062. doi: 10.1002/prp2.62. PMID: 25089200; PMCID: PMC4115637. 2: Xu X, Xu X, Hao Y, Zhu X, Lu J, Ouyang X, Lu Y, Huang X, Li Y, Wang J, Shen X. Antispasmodic Drug Drofenine as an Inhibitor of Kv2.1 Channel Ameliorates Peripheral Neuropathy in Diabetic Mice. iScience. 2020 Sep 28;23(10):101617. doi: 10.1016/j.isci.2020.101617. PMID: 33089105; PMCID: PMC7559245. 3: Bodur E, Cokuğraş AN, Tezcan EF. Inhibition effects of benactyzine and drofenine on human serum butyrylcholinesterase. Arch Biochem Biophys. 2001 Feb 1;386(1):25-9. doi: 10.1006/abbi.2000.2188. PMID: 11360997. 4: Yan L, Zhang X, Fu J, Liu Q, Lei X, Cao Z, Zhang J, Shao Y, Tong Q, Qin W, Liu X, Liu C, Liu Z, Li Z, Lu J, Xu X. Inhibition of the transient receptor potential vanilloid 3 channel attenuates carbon tetrachloride-induced hepatic fibrosis. Biochem Biophys Res Commun. 2021 Jun 18;558:86-93. doi: 10.1016/j.bbrc.2021.04.065. Epub 2021 Apr 24. PMID: 33906111. 5: Facchini G, Zaccheo F, Nannetti M. Simultaneous determination of hydrochloride salts of adiphenine, diphenhydramine, ethyldiphenacetate, drofenine and promazine by ion-pair HPLC. Boll Chim Farm. 1983 Aug;122(8):405-11. PMID: 6140928. 6: Kunysz EL, Michel AD, Whiting RL. Functional and direct binding studies using subtype selective muscarinic receptor antagonists. Br J Pharmacol. 1988 Mar;93(3):491-500. doi: 10.1111/j.1476-5381.1988.tb10303.x. PMID: 2897216; PMCID: PMC1853838. 7: Pawelczyk E, Hermann T, Marciniec B, Pluta I. Studies on kinetics of degradation of drugs. XIX. Thermic degradation of aminophenazone (AP), allobarbital (AB), cycloadiphenine hydrochloride (CAD) mixture in cetyl phtalate medium. Acta Pol Pharm. 1971;28(6):594-602. PMID: 5163824.