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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-42894

Umeclidinium bromide

mAChR antagonist

Umeclidinium bromide (GSK573719A) is potent, long-acting, inhaled antagonist of mAChRs with Ki of 0.05-0.16 nM for human M1-M5 mAChRs.
PC-63038

THRX-198321

MABA

THRX-198321 is a bifunctional mAChR antagonist and β2-adrenoceptor agonist (MABA) with pKi of 9.69/10.05 for M1/M2 respectively, pEC50 of 9.25 for β2AR.
PC-62746

ML375

M5 mAChR NAM

ML375 (VU0483253) is a potent, highly selective M5 NAM with submicromolar potency (human M5 IC50=300 nM, rat M5 IC50=790 nM, M1-M4 IC50> 30 uM).
PC-62161

VU0152099

M4 mAChR PAM

VU0152099 is a potent, selective, CNS-penetrant positive allosteric modulator of M4 mAChR with EC50 of 403 nM.
PC-62160

VU 10010

M4 mAChR PAM

VU 10010 is a selective, allosteric potentiator of M4 mAChR (EC50=33 and 0.7 nM for ACh in the absence and presence of VU10010 respectively), has no activity at other mAChR subtypes.
PC-62144

ML381 fumarate

M5 mAChR antagonist

ML381 (VU0488130) is a highly mAChR subtype selective M5 orthosteric antagonist with IC50/Ki of 450/340 nM for hM5, has no inhibitory activity on hM1-4 (IC50>30 uM).
PC-62143

ML381

M5 mAChR antagonist

ML381 (VU0488130) is a highly mAChR subtype selective M5 orthosteric antagonist with IC50/Ki of 450/340 nM for hM5, has no inhibitory activity on hM1-4 (IC50>30 uM).
PC-62140

VU0481443

M5 mAChR PAM

VU0481443 (ML380) is a potent, selective and CNS penetrant M5 positive allosteric modulator (PAM) with EC50 of 190 nM for hM5.
PC-62118

VU 6008667

M5 mAChR PAM

VU 6008667 is a potent, highly selective M5 negative allosteric modulator with IC50 of 1.2 uM.
PC-61894

PF-3635659

M3 mAChR antagonist

PF-3635659 (PF-03635659) is a potent, very long dissociative half-life (slow off-rate, >1440 min) muscarinic M3 antagonist with Ki of 0.2 nM, shows potential for the treatment of chronic obstructive pulmonary disease (COPD).
PC-61893

Fesoterodine fumarate

mAChR antagonist

Fesoterodine fumarate (PF-00695838) is a competitive muscarinic receptor antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors.
PC-61891

Fesoterodine

mAChR antagonist

Fesoterodine (PF-00695838) is a competitive muscarinic receptor antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors.

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