Description
nAChR agonist CMPI hydrochloride is a potent and selective positive allosteric modulator (PAM) of nAChR containing a α4:α4 subunit interface. nAChR agonist CMPI hydrochloride enhances the response of (α4)3(β2)2 nAChR to ACh (10 µM) with an EC50 of 0.26 µM. nAChR agonist CMPI hydrochloride has potential for the research of nicotine dependence and many neuropsychiatric conditions associated with decreased brain cholinergic activity.
Product information
CAS Number: 2250025-94-4
Molecular Weight: 379.28
Formula: C18H20Cl2N4O
Chemical Name: 4-{4-[3-(2-chlorophenyl)-1,2-oxazol-5-yl]-5-methyl-1H-pyrazol-1-yl}piperidine; chlorohydrogen
Smiles: Cl.CC1=C(C=NN1C1CCNCC1)C1=CC(=NO1)C1=CC=CC=C1Cl
InChiKey: WNKFVIPYZXTQBR-UHFFFAOYSA-N
InChi: InChI=1S/C18H19ClN4O.ClH/c1-12-15(11-21-23(12)13-6-8-20-9-7-13)18-10-17(22-24-18)14-4-2-3-5-16(14)19;/h2-5,10-11,13,20H,6-9H2,1H3;1H
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
CMPI (0.01-10 µM) potentiates (α4)3(β2)2 (low ACh sensitivity) but not (α4)2(β2)3 (high ACh sensitivity) nAChRs in Xenopus laevis oocytes. CMPI (0.01-10 µM) inhibits (α4)2(β2)3, human muscle and Torpedo nAChRs with IC50s of 0.6, 0.7 and 0.2 µM, respectively in Xenopus oocytes.
References:
- Hamouda AK, et, al. Photolabeling a Nicotinic Acetylcholine Receptor (nAChR) with an (α4)3(β2)2 nAChR-Selective Positive Allosteric Modulator. Mol Pharmacol. 2016 May;89(5):575-84.
- Wang ZJ, et, al. Unraveling amino acid residues critical for allosteric potentiation of (α4)3(β2)2-type nicotinic acetylcholine receptor responses. J Biol Chem. 2017 Jun 16;292(24):9988-10001.
Products are for research use only. Not for human use.
Payment & Security
Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.