This product is analyzed for solubility in DMSO on a lot to lot basis. The specification is: ≥ 20.0 mg/mL. Kindly review the lot specific certificate of analysis for the resulting maximum solubility of the lot received.
SML0800
利莫那班 盐酸盐
≥98% (HPLC), powder, cannabinoid type-I receptor antagonist
同義詞:
5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-1-piperidinyl-1H-pyrazole-3-carboxamide hydrochloride, SR-141716, SR-141716A, SR141716, SR141716A
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About This Item
經驗公式（希爾表示法）:
C22H21Cl3N4O · HCl
CAS號碼:
分子量：:
500.25
分類程式碼代碼:
12352200
PubChem物質ID:
NACRES:
NA.77
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產品名稱
利莫那班 盐酸盐, ≥98% (HPLC)
化驗
≥98% (HPLC)
形狀
powder
儲存條件
desiccated
顏色
white to beige
溶解度
DMSO: 20 mg/mL, clear
儲存溫度
2-8°C
SMILES 字串
CC1=C(C2=CC=C(Cl)C=C2)N(C3=CC=C(Cl)C=C3Cl)N=C1C(NN4CCCCC4)=O.Cl
InChI
1S/C22H21Cl3N4O.ClH/c1-14-20(22(30)27-28-11-3-2-4-12-28)26-29(19-10-9-17(24)13-18(19)25)21(14)15-5-7-16(23)8-6-15;/h5-10,13H,2-4,11-12H2,1H3,(H,27,30);1H
InChI 密鑰
REOYOKXLUFHOBV-UHFFFAOYSA-N
基因資訊
human ... CNR1(1268)
應用
Rimonabant hydrochloride has been used as an antagonist of cannabinoid 1 (CB1) receptor:
- to study its effects on protein synthesis in C2C12 myotubes[1]
- to analyze its effects on human astroglia[2]
- in combination with methanandamide (mAEA) to study its effects on murine gastric vagal afferent mechanosensitivity[3]
生化／生理作用
Rimonabant acts as a mycobacterial membrane protein large 3 (MMPL3) inhibitor.[4] Rimonabant hydrochloride exhibits therapeutic activity against weight reduction and smoking cessation.[5]
Rimonabant hydrochloride (SR-141716A) is a potent and selective CB1 cannabinoid inverse agonist/antagonist with a Ki of 1.6 nM, minimal affinity for CB2, and and some GPR55 agonist activity. Rimonabant was developed as an anti-obesity drug because of its appetite suppressant activity, but was taken off the market because of side effects of depression and anxiety.
Rimonabant hydrochloride (SR-141716A) is a potent and selecvtive CB1 cannabinoid inverse agonist/antagonist with some GPR55 agonist activity and an appetite suppressant.
特點和優勢
This compound is featured on the Cannabinoid Receptors and Cannabinoid Receptors pages of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
訊號詞
Danger
危險聲明
危險分類
Acute Tox. 3 Oral - Eye Irrit. 2
儲存類別代碼
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
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分析證明 (COA)
Lot/Batch Number
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Marc-Antoine Perrin et al.
Journal of pharmaceutical sciences, 102(7), 2311-2321 (2013-05-23)
Crystalline polymorphism occurs frequently in the solid state of active pharmaceutical ingredients, and this is problematic for the development of a suitable dose form. Rimonabant, an active pharmaceutical ingredient developed by Sanofi and discontinued because of side effects, exhibits dimorphism;
A novel validated RP-HPLC method development for the estimation of rimonabant hydrochloride in bulk and tablet dosage forms
Nama S, et al.
African Journal of Pharmacy and Pharmacology, 5(2), 207-213 (2011)
Jorge Emilio Ortega et al.
European journal of pharmacology, 709(1-3), 13-19 (2013-04-09)
Current pharmacological therapies for depression, including selective serotonin reuptake inhibitors (SSRI), are far from ideal. The cannabinoid system has been implicated in control of mood and neural processing of emotional information, and the modulation of serotonin (5-HT) release in the
Wei Chen et al.
Naunyn-Schmiedeberg's archives of pharmacology, 386(8), 721-732 (2013-04-27)
Effects of cannabinoid receptor 1 (CB1R) blockade were observed by comparing 9-day and 6-week SR141716 treatments in monosodium glutamate (MSG)-induced hypometabolic and hypothalamic obesity (HO) in rats for the first time and molecular mechanisms were investigated. Compared with normal rats
Erkan Kilinc et al.
The European journal of neuroscience, 55(4), 1015-1031 (2020-07-09)
Calcitonin gene-related peptide (CGRP), substance P and dural mast cells are main contributors in neurogenic inflammation underlying migraine pathophysiology. Modulation of endocannabinoid system attenuates migraine pain, but its mechanisms of action remain unclear. We investigated receptor mechanisms mediating anti-neuroinflammatory effects
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Hi ! In the product information its marked that rimonabant's solubility in DMSO is "20 mg/mL, clear". Is it its maximum solubility in DMSO?
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