| Bioactivity | VU10010 is a potent, highly selective and allosteric M4 mAChR potentiator with an EC50 of 400 nM. VU10010 binds to an allosteric site on M4 mAChR and increases affinity for acetylcholine and coupling to G proteins. VU10010 increases carbachol-induced depression of transmission at excitatory but not inhibitory synapses in the hippocampus[1]. | ||||||||||||
| Invitro | VU10010 potentiates the M4 response to acetylcholine 47-fold while having no activity at other mAChR subtypes (rM1, rM2, rM3 or rM5). VU10010 causes an increase in affinity for ACh and M4-mediated [35S]GTPγS binding[1]. VU10010 (10 μM) has no agonist, antagonist or allosteric potentiator activity at P2Y1R or mGluR5[1]. The EC50 values are 33 and 0.7 nM for ACh in the absence and presence of VU10010, respectively[1]. | ||||||||||||
| Name | VU10010 | ||||||||||||
| CAS | 633283-39-3 | ||||||||||||
| Formula | C17H16ClN3OS | ||||||||||||
| Molar Mass | 345.85 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Jana K Shirey, et al. An allosteric potentiator of M4 mAChR modulates hippocampal synaptic transmission. Nat Chem Biol. 2008 Jan;4(1):42-50. |
VU10010
CAS: 633283-39-3 F: C17H16ClN3OS W: 345.85
VU10010 is a potent, highly selective and allosteric M4 mAChR potentiator with an EC50 of 400 nM. VU10010 binds to an al
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