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首页-小分子抑制剂&激动剂-GPCR-mAChR

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Cat. No. Product Name Information
PC-23643

TAK‐071

M1 mAChR PAM

TAK-071 is a potent and highly selective positive allosteric modulator of M1 muscarinic acetylcholine receptor with EC50 of 520 nM.
PC-23642

BQCA

M1 mAChR PAM

BQCA is a highly selective positive allosteric modulator (PAM) of M1 mAChR with EC50 of 267 nM, shows high intrinsic M1 agonist activity.
PC-23641

VU0467319

M1 mAChR PAM

VU0467319 (VU319) is a potent, selective and CNS penetrant M1 mAChR positive allosteric modulator (PAM) with EC50 of 492 nM, with minimal M1 agonism (EC50 > 30 uM).
PC-23594

ADS10227

M2R/M4R antagonist

ADS10227 is a potent muscarinic receptor antagonist with binding Ki of 2.8 nM and 5.1 nM for human muscarinic M2 and M4 receptors (hM2R and hM4R) respectively.
PC-23358

BAY 2413555

M2 mAChR PAM

BAY 2413555 is a potent, selective positive allosteric modulator of M2 muscarinic acetylcholine receptor (M2 mAChR, M2R) with EC50 of 2.0 nM in functional M2-GIRK assays.
PC-23330

Pirenzepine

M1 mAChR antagonist

Pirenzepine (LS519, Pirenzepin, Gastrozepin) is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist, shows gastric secretion-inhibitory action but without central-nervous sedation.
PC-23023

Darifenacin

CHI3L1 inhibitor, M3 mAChR inhibitor

Darifenacin (UK-88525) is a potent, selective M3 muscarinic receptor antagonist with pKi of 8.9, also inhibits CHI3L1(Chitinase 3-like 1) and PDAC cell growth.
PC-22961

VU6007496

M1 mAChR PAM

VU6007496 is a highly selective and CNS penetrant M1 mAChR positive allosteric modulator (PAM) with EC50 of 228 nM (hM1), with minimal M1 agonism (EC50>10 μM).
PC-22893

VU6036864

M5 mAChR antagonist

VU6036864 is a highly potent, selective antagonist of muscarinic acetylcholine receptor mAChR subtype 5 (M5) with IC50 of 25 nM (hM5), >500 fold selectivity against M1-4 receptors.
PC-22795

PIPE-307

M1 mAChR antagonist

PIPE-307 is a potent, selective, orally bioavailable, brain-penetrant antagonist of M1 muscarinic acetylcholine receptor (M1R, M1 mAChR) with Ki of 4.6 nM in membranes overexpressing human M1R.
PC-22509

CHF-6550

MABA

CHF-6550 is a potent, dual acting muscarinic M3 antagonist and β2 agonist (MABA) with pKi values of 9.3 and 10.6 for M3 and β2 receptor, respectively.
PC-21369

VU 0365114

M5 mAChR PAM

VU 0365114 is a selective type-5 muscarinic acetylcholine receptor (mAChR, M5) positive allosteric modulator (EC50=2.7 uM) and tubulin inhibitor by destabilizing microtubules, shows no activity against M1, M2, M3 and M4 receptors.

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