4-Piperidinemethanamine, 1-[5,6,7,8-tetrahydro-2-(4-pyridinyl)[1]benzothieno[2,3-d]pyrimidin-4-yl]-
- CAS No.
- 2636771-29-2
- Chemical Name:
- 4-Piperidinemethanamine, 1-[5,6,7,8-tetrahydro-2-(4-pyridinyl)[1]benzothieno[2,3-d]pyrimidin-4-yl]-
- Synonyms
- PKC-IN-4;4-Piperidinemethanamine, 1-[5,6,7,8-tetrahydro-2-(4-pyridinyl)[1]benzothieno[2,3-d]pyrimidin-4-yl]-
- CBNumber:
- CB512617406
- Molecular Formula:
- C21H25N5S
- Molecular Weight:
- 379.52
- MDL Number:
- MOL File:
- 2636771-29-2.mol
4-Piperidinemethanamine, 1-[5,6,7,8-tetrahydro-2-(4-pyridinyl)[1]benzothieno[2,3-d]pyrimidin-4-yl]- Chemical Properties,Uses,Production
Uses
PKC-IN-4 (compound 7l) is a potent and orally active aPKC inhibitor with an IC50 of 0.52 μM. PKC-IN-4 inhibits TNF-α induced NF-κB activity in vitro. PKC-IN-4 blocks VEGF- and TNFα-induced permeability across the retinal vasculature[1].
in vivo
PKC-IN-4 (10 mg/kg for i.v.; 20 mg/kg for p.o.) shows orally active with oral bioavailability of 81.7%[1].
Animal Model: | Animal Model: CD-1 mice[1] |
Dosage: | 10, 20 mg/kg |
Administration: | 10 mg/kg for i.v.; 20 mg/kg for p.o. |
Result: | Showed good PK parameters with oral bioavailability of 81.7%. |
IC 50
PKC: 0.52 μM (IC50)
References
[1] Liu X, et al. Synthesis and structure-activity relationships of thieno[2,3-d]pyrimidines as atypical protein kinase C inhibitors to control retinal vascular permeability and cytokine-induced edema. Bioorg Med Chem. 2020 Jun 1;28(11):115480. DOI:10.1016/j.bmc.2020.115480
4-Piperidinemethanamine, 1-[5,6,7,8-tetrahydro-2-(4-pyridinyl)[1]benzothieno[2,3-d]pyrimidin-4-yl]- Preparation Products And Raw materials
Raw materials
Preparation Products
4-Piperidinemethanamine, 1-[5,6,7,8-tetrahydro-2-(4-pyridinyl)[1]benzothieno[2,3-d]pyrimidin-4-yl]- Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
TargetMol Chemicals Inc. | +17819995354 | marketing@targetmol.com | United States | 19904 | 58 |
TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 21549 | 58 |
Supplier | Advantage |
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TargetMol Chemicals Inc. | 58 |
TargetMol Chemicals Inc. | 58 |