Introduction：Basic information about CAS 452342-67-5|GW788388, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | GW788388 |
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| CAS Number | 452342-67-5 | Molecular Weight | 425.482 |
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| Density | 1.3±0.1 g/cm3 | Boiling Point | 683.2±55.0 °C at 760 mmHg |
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| Molecular Formula | C25H23N5O2 | Melting Point | / |
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| MSDS | / | Flash Point | 367.0±31.5 °C |
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Names
| Name | 4-(4-(3-(Pyridin-2-yl)-1H-pyrazol-4-yl)pyridin-2-yl)-N-(tetrahydro-2H-pyran-4-yl)benzamide |
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| Synonym | More Synonyms |
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GW788388 BiologicalActivity
| Description | GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, and also inhibits TGF-β type II receptor and activin type II receptor activities, without inhibiting BMP type II receptor. |
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| Related Catalog | Signaling Pathways >>TGF-beta/Smad >>TGF-β ReceptorResearch Areas >>Cancer |
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| Target | IC50: 18 nM (ALK5) |
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| In Vivo | GW788388 given orally for 5 weeks significantly reduces renal fibrosis and decreased the mRNA levels of key mediators of extracellular matrix deposition in kidneys in db/db mice[1]. GW788388 (50 mg/kg/day, p.o.) significantly attenuates systolic dysfunction in the MI animals, together with the attenuation of the activated (phosphorylated) Smad2 (P < 0.01), α-smooth muscle actin (P < 0.001), and collagen I (P < 0.05) in the noninfarct zone of MI rats[2]. GW788388 reduces the expression of collagen IA1 by 80% at a dose of 1 mg/kg twice a day (b.i.d.). GW788388 significantly reduces the expression of collagen IA1 mRNA when administered orally at 10 mg/kg once a day (u.i.d.) in a model of puromycin aminonucleoside-induced renal fibrosis[3]. |
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| Animal Admin | One week postsurgery, sham-operated (N=6) and infarcted animals (N=10) are randomized to treatment with the ALK5 inhibitor GW788388 (GSK) at a dosage of 50 mg/kg/day by gavage, which has been shown to significantly attenuate collagen overexpression in a rodent model of dimethylnitrosamine-induced liver disease. Untreated rats, that is, sham-operated (N=9) and MI animals (N=15), are gavaged with vehicle (1% carboxymethyl cellulose solution). Four animals with < 25% infarct size as determined postmortem by histology are excluded from further analyses. |
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| References | [1]. Petersen M, et al. Oral administration of GW788388, an inhibitor of TGF-beta type I and II receptor kinases, decreases renal fibrosis. Kidney Int, 2008, 73(6), 705-715. [2]. Tan SM, et al. Targeted inhibition of activin receptor-like kinase 5 signaling attenuates cardiac dysfunction following myocardial infarction. Am J Physiol Heart Circ Physiol, 2010, 298(5), H1415-1425. [3]. Gellibert F, et al. Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor. J Med Chem. 2006, 49 |
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Chemical & Physical Properties
| Density | 1.3±0.1 g/cm3 |
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| Boiling Point | 683.2±55.0 °C at 760 mmHg |
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| Molecular Formula | C25H23N5O2 |
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| Molecular Weight | 425.482 |
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| Flash Point | 367.0±31.5 °C |
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| Exact Mass | 425.185181 |
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| PSA | 92.79000 |
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| LogP | 1.88 |
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| Appearance of Characters | white solid |
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| Vapour Pressure | 0.0±2.1 mmHg at 25°C |
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| Index of Refraction | 1.680 |
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| InChIKey | SAGZIBJAQGBRQA-UHFFFAOYSA-N |
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| SMILES | O=C(NC1CCOCC1)c1ccc(-c2cc(-c3cn[nH]c3-c3ccccn3)ccn2)cc1 |
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| Storage condition | -20℃ |
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Safety Information
Customs
| HS Code | 2934999090 |
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| Summary | 2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
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Synonyms
| N-(oxan-4-yl)-4-[4-(5-pyridin-2-yl-1H-pyrazol-4-yl)pyridin-2-yl]benzamide |
| 4-{4-[5-(2-Pyridinyl)-1H-pyrazol-4-yl]-2-pyridinyl}-N-(tetrahydro-2H-pyran-4-yl)benzamide |
| 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H-pyran-4-yl)benzamide |
| Benzamide, 4-[4-[5-(2-pyridinyl)-1H-pyrazol-4-yl]-2-pyridinyl]-N-(tetrahydro-2H-pyran-4-yl)- |
| GW788388 |
