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

MedKoo CAT#: 318185

CAS#: 76-90-4

Description: Mepenzolate Bromide is a muscarinic antagonist used to treat gastrointestinal disorders. It decreases the severity of elastase-induced airspace enlargement and respiratory dysfunction.

Chemical Structure

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Mepenzolate Bromide
CAS# 76-90-4
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 318185
Name: Mepenzolate Bromide
CAS#: 76-90-4
Chemical Formula: C21H26BrNO3
Exact Mass: 0.00
Molecular Weight: 420.347
Elemental Analysis: C, 60.00; H, 6.23; Br, 19.01; N, 3.33; O, 11.42

Price and Availability

Size Price Availability Quantity
500mg USD 250 2 Weeks
100mg USD 450 2 Weeks
1g USD 750 2 weeks
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Synonym: Mepenzolate Bromide; Cantil; Gastropidil; Cantilaque; Cantilon; mepenzolate iodide; mepenzolic acid;

IUPAC/Chemical Name: (1,1-dimethylpiperidin-1-ium-3-yl) 2-hydroxy-2,2-diphenylacetate;bromide

InChi Key: JRRNZNSGDSFFIR-UHFFFAOYSA-M

InChi Code: InChI=1S/C21H26NO3.BrH/c1-22(2)15-9-14-19(16-22)25-20(23)21(24,17-10-5-3-6-11-17)18-12-7-4-8-13-18;/h3-8,10-13,19,24H,9,14-16H2,1-2H3;1H/q+1;/p-1

SMILES Code: C[N+]1(CCCC(C1)OC(=O)C(C2=CC=CC=C2)(C3=CC=CC=C3)O)C.[Br-]

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, not in water

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: Mepenzolate Bromide is a muscarinic antagonist.
In vitro activity: In this study’s attempt to isolate the pharmacologically active ingredients in the aqueous extracts of Mareya micrantha, this study has selected the contractions of the longitudinal muscle of the isolated guinea-pig ileum preparation as a pharmacological marker to monitor retention of pharmacological activity during the chromatographic separation. Mepenzolate (10(-8)-10(-5) M), a specific muscarinic receptor antagonist, similarly antagonized contractions elicited by the aqueous extracts suggesting that the cholinergic ingredient(s) in the extract are acting at the muscarinic receptors of the preparation. Reference: J Ethnopharmacol. 1995 Mar;45(3):215-22. https://pubmed.ncbi.nlm.nih.gov/7623487/
In vivo activity: The present study aimed at exploring the effect of niacin on experimental colitis in rats as well as throwing some light on the ability of niacin to modulate angiogenesis which plays a crucial role of in the pathogenesis of inflammatory bowel disease. Mepenzolate bromide, a GPR109A receptor blocker, abolished the beneficial effects of niacin on body weight, colon wet weight as well as colonic levels of MPO and VEGF. Reference: Sci Rep. 2017 Aug 2;7(1):7139. https://pubmed.ncbi.nlm.nih.gov/28769047/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMF 5.0 11.89
DMSO 30.0 71.37
PBS (pH 7.2) 1.0 2.38

Preparing Stock Solutions

The following data is based on the product molecular weight 420.35 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. Tsai CS, Guede-Guina F, Smith MO, Vangah-Manda M, Ochillo RF. Isolation of cholinergic active ingredients in aqueous extracts of Mareya micrantha using the longitudinal muscle of isolated guinea-pig ileum as a pharmacological activity marker. J Ethnopharmacol. 1995 Mar;45(3):215-22. doi: 10.1016/0378-8741(94)01219-p. PMID: 7623487. 2. Tsai CS, Ochillo RF. Low temperature and muscarinic receptor activities. Cryobiology. 1989 Oct;26(5):485-95. doi: 10.1016/0011-2240(89)90072-2. PMID: 2791613. 3. Salem HA, Wadie W. Effect of Niacin on Inflammation and Angiogenesis in a Murine Model of Ulcerative Colitis. Sci Rep. 2017 Aug 2;7(1):7139. doi: 10.1038/s41598-017-07280-y. PMID: 28769047; PMCID: PMC5541000. 4. Zheng Y, Wang X, Ji S, Tian S, Wu H, Luo P, Fang H, Wang L, Wu G, Xiao S, Xia Z. Mepenzolate bromide promotes diabetic wound healing by modulating inflammation and oxidative stress. Am J Transl Res. 2016 Jun 15;8(6):2738-47. PMID: 27398156; PMCID: PMC4931167.
In vitro protocol: 1. Tsai CS, Guede-Guina F, Smith MO, Vangah-Manda M, Ochillo RF. Isolation of cholinergic active ingredients in aqueous extracts of Mareya micrantha using the longitudinal muscle of isolated guinea-pig ileum as a pharmacological activity marker. J Ethnopharmacol. 1995 Mar;45(3):215-22. doi: 10.1016/0378-8741(94)01219-p. PMID: 7623487. 2. Tsai CS, Ochillo RF. Low temperature and muscarinic receptor activities. Cryobiology. 1989 Oct;26(5):485-95. doi: 10.1016/0011-2240(89)90072-2. PMID: 2791613.
In vivo protocol: 1. Salem HA, Wadie W. Effect of Niacin on Inflammation and Angiogenesis in a Murine Model of Ulcerative Colitis. Sci Rep. 2017 Aug 2;7(1):7139. doi: 10.1038/s41598-017-07280-y. PMID: 28769047; PMCID: PMC5541000. 2. Zheng Y, Wang X, Ji S, Tian S, Wu H, Luo P, Fang H, Wang L, Wu G, Xiao S, Xia Z. Mepenzolate bromide promotes diabetic wound healing by modulating inflammation and oxidative stress. Am J Transl Res. 2016 Jun 15;8(6):2738-47. PMID: 27398156; PMCID: PMC4931167.

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1: Yamashita Y, Tanaka K, Asano T, Yamakawa N, Kobayashi D, Ishihara T, Hanaya K,
Shoji M, Sugai T, Wada M, Mashimo T, Fukunishi Y, Mizushima T. Synthesis and
biological comparison of enantiomers of mepenzolate bromide, a muscarinic
receptor antagonist with bronchodilatory and anti-inflammatory activities. Bioorg
Med Chem. 2014 Jul 1;22(13):3488-97. doi: 10.1016/j.bmc.2014.04.029. Epub 2014
Apr 30. PubMed PMID: 24844758.


2: Kurotsu S, Tanaka K, Niino T, Asano T, Sugizaki T, Azuma A, Suzuki H,
Mizushima T. Ameliorative effect of mepenzolate bromide against pulmonary
fibrosis. J Pharmacol Exp Ther. 2014 Jul;350(1):79-88. doi:
10.1124/jpet.114.213009. Epub 2014 Apr 25. PubMed PMID: 24769542.


3: Tanaka K, Kurotsu S, Asano T, Yamakawa N, Kobayashi D, Yamashita Y, Yamazaki
H, Ishihara T, Watanabe H, Maruyama T, Suzuki H, Mizushima T. Superiority of
pulmonary administration of mepenzolate bromide over other routes as treatment
for chronic obstructive pulmonary disease. Sci Rep. 2014 Mar 28;4:4510. doi:
10.1038/srep04510. PubMed PMID: 24676126; PubMed Central PMCID: PMC3968453.


4: Tanaka K, Ishihara T, Sugizaki T, Kobayashi D, Yamashita Y, Tahara K, Yamakawa
N, Iijima K, Mogushi K, Tanaka H, Sato K, Suzuki H, Mizushima T. Mepenzolate
bromide displays beneficial effects in a mouse model of chronic obstructive
pulmonary disease. Nat Commun. 2013;4:2686. doi: 10.1038/ncomms3686. PubMed PMID:
24189798.


5: Mepenzolate bromide in mucomembranous colitis. A report from the General
Practitioner research group. Practitioner. 1974 Jun;212(1272):890-4. PubMed PMID:
4608714.


6: Friedman HL, Wang RI. Oral absorption of 14 C-labeled mepenzolate bromide in
humans. J Pharm Sci. 1972 Oct;61(10):1663-5. PubMed PMID: 5072426.