| Company Name: |
TargetMol Chemicals Inc.
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| Tel: |
15002134094 |
| Email: |
marketing@targetmol.cn |
| Products Intro: |
Product Name:DprE1-IN-4
CAS:2419160-96-4
Package:25mg/RMB 10600;100mg/RMB 17500;50mg/RMB 13800
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Carbamic acid, N-[[2-[[4-(1-piperidinylcarbonyl)benzoyl]amino]-3-thienyl]carbonyl]-, methyl ester manufacturers
- DprE1-IN-4
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- $1520.00 / 25mg
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2025-10-27
- CAS:2419160-96-4
- Min. Order:
- Purity:
- Supply Ability: 10g
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| | Carbamic acid, N-[[2-[[4-(1-piperidinylcarbonyl)benzoyl]amino]-3-thienyl]carbonyl]-, methyl ester Basic information |
| | Carbamic acid, N-[[2-[[4-(1-piperidinylcarbonyl)benzoyl]amino]-3-thienyl]carbonyl]-, methyl ester Chemical Properties |
| density | 1.370±0.06 g/cm3(Predicted) | | pka | 10.11±0.46(Predicted) |
| | Carbamic acid, N-[[2-[[4-(1-piperidinylcarbonyl)benzoyl]amino]-3-thienyl]carbonyl]-, methyl ester Usage And Synthesis |
| Uses | DprE1-IN-4 is a potent and orally active noncovalent DprE1 inhibitor with an IC50 of 0.90 μg/mL. DprE1-IN-4 exhibits potent in vitro activity against M. tuberculosis H37Rv and drug-resistant tuberculosis strain with MIC values of 0.12 μg/mL and 0.24 μg/mL, respectively. DprE1-IN-4 displays acceptable pharmacokinetic property and shows significant bactericidal activity in an acute mouse model of tuberculosis. | | in vivo | DprE1-IN-4 exhibits acceptable pharmacokinetic property after p.o. and i.v., DprE1-IN-4 (oral administration, 50 mg/kg) exhibits high plasma exposure ((AUC)0-∞=657 ng·h/mL) and high maximum plasma concentration (Cmax=486 ng/mL). It exhibits oral bioavailability (F=7.9%) and is deemed worthy of further evaluation in?in vivo?efficacy studies[1].DprE1-IN-4 (oral gavage; 100 mg/kg; once daily; 3 weeks) showed potent?in vivo?activity, reducing the bacterial burden in the lungs by 2.02?log10?CFU compared with the untreated control group[1]. | | References | [1] Pengxu Wang, et al. Discovery of Novel Thiophene-arylamide Derivatives as DprE1 Inhibitors with Potent Antimycobacterial Activities. J Med Chem. 2021 May 13;64(9):6241-6261. DOI:10.1021/acs.jmedchem.1c00263 |
| | Carbamic acid, N-[[2-[[4-(1-piperidinylcarbonyl)benzoyl]amino]-3-thienyl]carbonyl]-, methyl ester Preparation Products And Raw materials |
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