1. GPCR/G Protein Neuronal Signaling
  2. mAChR
  3. VU6007678

VU6007678 (compound 18g) is a central nervous system-penetrant muscarinic acetylcholine receptor(mAChR) potentiator. VU6007678 potentiates acetylcholine-mediated signaling at human M1, M3, M5 and rat M1, M3, M4, M5 muscarinic acetylcholine receptors. VU6007678 is applicable to research related to Alzheimer's disease, schizophrenia, and ischemic stroke.

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VU6007678

VU6007678 Chemical Structure

CAS No. : 2222737-15-5

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Description

VU6007678 (compound 18g) is a central nervous system-penetrant muscarinic acetylcholine receptor(mAChR) potentiator. VU6007678 potentiates acetylcholine-mediated signaling at human M1, M3, M5 and rat M1, M3, M4, M5 muscarinic acetylcholine receptors. VU6007678 is applicable to research related to Alzheimer's disease, schizophrenia, and ischemic stroke[1].

In Vitro

VU6007678 (10-point serial dilutions starting at 30 μM; 2.5 min with cells, 1 min with EC20 acetylcholine) potently acts as a positive allosteric modulator of human M5 receptors expressed in CHO cells, with an EC50 of 41 nM and a maximum response of 74% of acetylcholine's peak activity[1].
VU6007678 (10-point serial dilutions starting at 30 μM; 2.5 min with cells, 1 min with EC20 acetylcholine) acts as a positive allosteric modulator of rat M5 receptors expressed in CHO cells, with an EC50 of 74 nM and a maximum response of 76% of acetylcholine's peak activity[1].
VU6007678 (10-point serial dilutions starting at 30 μM; 2.5 min with cells, 1 min with EC20 acetylcholine) acts as a positive allosteric modulator of human M1 receptors expressed in CHO cells, with an EC50 of 1034 nM and a maximum response of 67% of acetylcholine's peak activity[1].
VU6007678 (10-point serial dilutions starting at 30 μM; 2.5 min with cells, 1 min with EC20 acetylcholine) acts as a positive allosteric modulator of human M3 receptors expressed in CHO cells, with an EC50 of 466 nM and a maximum response of 71% of acetylcholine's peak activity[1].
VU6007678 (10-point serial dilutions starting at 30 μM; 2.5 min with cells, 1 min with EC20 acetylcholine) acts as a positive allosteric modulator of rat M1 receptors expressed in CHO cells, with an EC50 of 904 nM and a maximum response of 69% of acetylcholine's peak activity[1].
VU6007678 (10-point serial dilutions starting at 30 μM; 2.5 min with cells, 1 min with EC20 acetylcholine) acts as a positive allosteric modulator of rat M3 receptors expressed in CHO cells, with an EC50 of 772 nM and a maximum response of 51% of acetylcholine's peak activity[1].
VU6007678 (10-point serial dilutions starting at 30 μM; 2.5 min with cells, 1 min with EC20 acetylcholine) weakly acts as a positive allosteric modulator of rat M4 receptors expressed in CHO cells, with an EC50 of 3913 nM and a maximum response of 49% of acetylcholine's peak activity[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Parmacokinetics
Species Dose Route CLplasma
Rat[1] 0.20-0.25 mg/kg i.v. > 60 mL/min/kg
Rat[1] 0.20-0.25 mg/kg i.p. > 60 mL/min/kg
Molecular Weight

484.59

Formula

C25H29FN4O3S

CAS No.
SMILES

N(C(=O)C1CCN(S(=O)(=O)C=2C=C3C(=CC2)NN=C3)CC1)(CCC)[C@H]4C=5C(CC4)=C(F)C=CC5

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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VU6007678
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