af-353
Modify Date: 2024-01-09 12:12:43
af-353 structure
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Common Name | af-353 | ||
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| CAS Number | 865305-30-2 | Molecular Weight | 400.21500 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C14H17IN4O2 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of af-353AF-353 is a novel, potent and orally bioavailable P2X3/P2X2/3 receptor antagonist, inhibits human and rat P2X3 (pIC50= 8.0).IC50 value: pIC50 = 8.0 (pIC50, for P2X3)Target: P2X3/P2X2/3 receptorin vitro: AF-353 is a highly potent inhibitor of α,β-meATP-evoked intracellular calcium flux in cell lines expressing recombinant rat and human P2X3 and human P2X2/3 channels. AF-353 also blocks human P2X2/3 channel function with marginally reduced potency (pIC50 = 7.3). [1]in vivo: SCI rats has significantly higher frequencies for field potentials and NVC than NL rats. Intravesical ATP increases field potential frequency in control but not SCI rats, while systemic AF-353 significantly reduces this parameter in both groups. AF-353 also reduces the inter-contractile interval in control but not in SCI rats; however, the frequency of NVC in SCI rats was significantly reduced.[2] |
| Name | 5-(5-iodo-4-methoxy-2-propan-2-ylphenoxy)pyrimidine-2,4-diamine |
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| Synonym | More Synonyms |
| Description | AF-353 is a novel, potent and orally bioavailable P2X3/P2X2/3 receptor antagonist, inhibits human and rat P2X3 (pIC50= 8.0).IC50 value: pIC50 = 8.0 (pIC50, for P2X3)Target: P2X3/P2X2/3 receptorin vitro: AF-353 is a highly potent inhibitor of α,β-meATP-evoked intracellular calcium flux in cell lines expressing recombinant rat and human P2X3 and human P2X2/3 channels. AF-353 also blocks human P2X2/3 channel function with marginally reduced potency (pIC50 = 7.3). [1]in vivo: SCI rats has significantly higher frequencies for field potentials and NVC than NL rats. Intravesical ATP increases field potential frequency in control but not SCI rats, while systemic AF-353 significantly reduces this parameter in both groups. AF-353 also reduces the inter-contractile interval in control but not in SCI rats; however, the frequency of NVC in SCI rats was significantly reduced.[2] |
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| Related Catalog | |
| References |
| Molecular Formula | C14H17IN4O2 |
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| Molecular Weight | 400.21500 |
| Exact Mass | 400.04000 |
| PSA | 97.74000 |
| LogP | 3.03010 |
|
~94%
af-353 CAS#:865305-30-2 |
| Literature: Roche Palo Alto LLC Patent: US2007/49609 A1, 2007 ; Location in patent: Page/Page column 87-88 ; US 20070049609 A1 |
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~%
af-353 CAS#:865305-30-2 |
| Literature: Carter, David S.; Alam, Muzaffar; Cai, Haiying; Dillon, Michael P.; Ford, Anthony P.D.W.; Gever, Joel R.; Jahangir, Alam; Lin, Clara; Moore, Amy G.; Wagner, Paul J.; Zhai, Yansheng Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 6 p. 1628 - 1631 |
| Precursor 2 | |
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| DownStream 1 | |
CAS#:865304-65-0| af-353 |
| 2,4-PyriMidinediaMine, 5-[5-iodo-4-Methoxy-2-(1-Methylethyl)phenoxy]- |