| Identification | Back Directory | [Name]
Carbamic acid, N-[3-[3-[(1R)-1-[cyclopropyl[(2R)-2-morpholinylcarbonyl]amino]ethyl]-6-methyl-1H-pyrazolo[3,4-b]pyridin-1-yl]propyl]-, methyl ester | [CAS]
1399849-02-5 | [Synonyms]
SPH3127
N-[3-[3-[(1R)-1-[cyclopropyl-[[(2R)-2-morpholinyl]-oxomethyl]amino]ethyl]-6-methyl-1-pyrazolo[3,4-b]pyridinyl]propyl]carbamic acid methyl ester
Carbamic acid, N-[3-[3-[(1R)-1-[cyclopropyl[(2R)-2-morpholinylcarbonyl]amino]ethyl]-6-methyl-1H-pyrazolo[3,4-b]pyridin-1-yl]propyl]-, methyl ester | [Molecular Formula]
C22H32N6O4 | [MOL File]
1399849-02-5.mol | [Molecular Weight]
444.53 |
| Chemical Properties | Back Directory | [Boiling point ]
667.4±55.0 °C(Predicted) | [density ]
1.39±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
12.38±0.46(Predicted) | [color ]
Off-white to pink |
| Hazard Information | Back Directory | [Uses]
SPH3127 (DRI 18) is a novel, highly potent, and orally active direct renin inhibitor (recombinant human-renin IC50=0.4 nM, human plasma renin activity IC50=0.45 nM). SPH3127 shows antihypertensive effect and can be used in essential hypertension research[1]. | [in vivo]
SPH3127 (oral administration; 0-10 mg/kg; once) shows favorable bioavailability in cynomolgus monkeys[1].
SPH3127 (oral administration; 0-3 mg/kg; once) shows a hypotensive effect on tsukuba hypertensive mice[1]. | Animal Model: | Cynomolgus monkeys pretreated with a low-sodium diet and furosemide[1] | | Dosage: | 0, 1, 3, and 10 mg/kg | | Administration: | Oral administration; 1, 3, and 10 mg/kg; once | | Result: | Inhibited plasma renin activity with the IC50 value of 0.46 nM, and showed hypotensive effect. |
| Animal Model: | Tsukuba hypertensive mice (THM)[1] | | Dosage: | 0, 0.3, 1, or 3 mg/kg | | Administration: | Oral administration; 0, 0.3, 1, or 3 mg/kg; once | | Result: | Exhibited a hypotensive effect on tsukuba hypertensive mice in a dose-dependent manner from 0.3 to 3 mg/kg, and showed a maximum hypotensive effect of approximately 30 mmHg at 2-3 h after administration at any dose. |
| [References]
[1] Daisuke Iijima, et al. Discovery of SPH3127: A Novel, Highly Potent, and Orally Active Direct Renin Inhibitor. J Med Chem. 2022 Aug 8. DOI:10.1021/acs.jmedchem.2c00834 |
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| Company Name: |
ChemOrigin Pharm
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021-15026428026 15026428026 |
| Website: |
chemorigin.com/ |
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