VU0467154
Modify Date: 2024-01-10 20:53:32
VU0467154 structure
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Common Name | VU0467154 | ||
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| CAS Number | 1451993-15-9 | Molecular Weight | 444.45100 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C17H15F3N4O3S2 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of VU0467154VU0467154 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor (mAChR), potentiating the response to ACh with pEC50s of 7.75, 6.2 and 6 for rat, human and cynomolgus monkey M4 receptor, respectively. |
| Name | 5-amino-3,4-dimethyl-N-(4-((trifluoromethyl)sulfonyl)benzyl)thieno-[2,3-c]pyridazine-6-carboxamide |
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| Synonym | More Synonyms |
| Description | VU0467154 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor (mAChR), potentiating the response to ACh with pEC50s of 7.75, 6.2 and 6 for rat, human and cynomolgus monkey M4 receptor, respectively. |
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| Related Catalog | |
| Target |
pEC50: of 7.75 (Rat M4 receptor), 6.2 (Human M4 receptor), 6 (Cynomolgus monkey M4 receptor)[1] |
| In Vitro | VU0467154 is a positive allosteric modulators of the M4 muscarinic acetylcholine receptor (mAChR), robustly potentiates the response to ACh with pEC50s of 7.75, 6.2 and 6 for rat, human and cynomolgus monkey (cyno) M4 receptor, respectively. VU0467154 does not potentiate the ACh response at rat and human M1, M2, M3, or M5[1]. |
| In Vivo | VU0467154 (1-56.6 mg/kg, p.o. or i.p.) reverses amphetamine-induced hyperlocomotion in rats. VU0467154 (0.3-30 mg/kg, i.p.) reverses amphetamine- and MK-801-induced hyperlocomotion in wild-type but not M4 KO mice. VU0467154 alone also enhances the acquisition of both contextual and cue-mediated fear conditioning in wild-type mice[1]. |
| Animal Admin | Rats[1] To determine the relationship between in vivo efficacy of VU0467154 and brain concentrations in rats, the efficacy of VU0467154 (1, 3, 10, 30, and 56.6 mg/kg, PO; n ≥ 8 per dose level) in reversing amphetamine-induced hyperlocomotion is correlated to the brain concentrations of VU0467154 in the same animals upon study completion (1.5 h postadministration). In mice, the in vivo concentration-effect relationship for VU0467154 is determined by correlating the efficacy of VU0467154 in reversing amphetamine-induced hyperlocomotion (0.3, 1, 3, 10, and 30 mg/kg, IP) to the brain concentrations of VU0467154 in the same animals upon study completion (2.5 h postadministration). Terminal unbound brain concentrations for all treatment groups are plotted versus each animal’s efficacy in reversing amphetamine-induced hyperlocomotion. Nonlinear regression analysis of the plotted data are calculated to determine the in vivo EC50 value (nM) for VU0467154 in reversing amphetamine-induced hyperlocomotion in rats using GraphPad Prism 5.0[1]. |
| References |
| Molecular Formula | C17H15F3N4O3S2 |
|---|---|
| Molecular Weight | 444.45100 |
| Exact Mass | 444.05400 |
| PSA | 151.66000 |
| LogP | 5.16670 |
| Storage condition | 2-8℃ |
| VU0467154 |
| 5-amino-3,4-dimethyl-N-(4-((trifluoromethyl)sulfonyl)benzyl)thieno[2,3-c]pyridazine-6-carboxamide |
- Shanghai Nianxing Industrial Co., Ltd
- China
- Product Name: VU0467154?
- Price: Negotiable
- Purity: 98.0%
- Delivery: 10 Day
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- DC Chemicals Limited
- China
- Product Name: VU0467154
- Price: $Inquiry/100mg $Inquiry/250mg $Inquiry/1g
- Purity: 98.0%
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- ShangHai DC Chemicals Co.,Ltd
- China
- Product Name: VU0467154
- Price: ￥Inquiry/1g
- Purity: 98.9%
- Delivery: 1 Day
- Contact: Tony Lai
- Email: order@dcchemicals.com
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