A 33 manufacturers
- PDE4B-IN-2
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- $31.00 / 1mg
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2025-11-10
- CAS:915082-52-9
- Min. Order:
- Purity: 99.37%
- Supply Ability: 10g
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| Product Name: | A 33 | | Synonyms: | A-33;Benzeneacetic acid, 4-[[2-(5-chloro-2-thienyl)-5-ethyl-6-methyl-4-pyrimidinyl]amino]-;PDE4B-IN-2;2-(4-{[2-(5-chlorothiophen-2-yl)-5-ethyl-6-methylpyrimidin-4-yl]amino}phenyl)acetic acid;PDE4B-IN-2, 10 mM in DMSO | | CAS: | 915082-52-9 | | MF: | C19H18ClN3O2S | | MW: | 387.88 | | EINECS: | | | Product Categories: | | | Mol File: | 915082-52-9.mol |  |
| storage temp. | Store at -20°C | | solubility | 38.7mg/ml in DMSO | | form | Solid | | color | White to off-white | | InChI | InChI=1S/C19H18ClN3O2S/c1-3-14-11(2)21-19(15-8-9-16(20)26-15)23-18(14)22-13-6-4-12(5-7-13)10-17(24)25/h4-9H,3,10H2,1-2H3,(H,24,25)(H,21,22,23) | | InChIKey | FDVSPBLZPJMXFV-UHFFFAOYSA-N | | SMILES | C1(CC(O)=O)=CC=C(NC2C(CC)=C(C)N=C(C3SC(Cl)=CC=3)N=2)C=C1 |
| Uses | PDE4B-IN-2 is an orally active and selective PDE4B inhibitor with an IC50 of 15 nM. PDE4B-IN-2 inhibits PDE4D (IC50=1.7 μM). PDE4B-IN-2 exhibits potent anti-inflammatory effects[1]. | | Biochem/physiol Actions | A-33 (A33) is a potent and selective catalytic site-targeting PDE4B inhibitor (IC50 = 15 nM/PDE4B vs. 1.7 μM/PDE4D) that effectively prevents PDE4B-medicated cellular cAMP hydrolysis (150%/320% increased cAMP level with 100 nM/1 μM A-33 pre-treament in murine hippocampal HT-22 cells following 10 nM isoproterenol stimulation) in vitro and inhibits LPS-induced TNF-α production in mice in vivo (ID50 = 14 mg/kg p.o.). When administered via intraperitoneal injection, A-33 improves cognitive function in a rat model of traumatic brain injury (0.3 mg/kg i.p.) and exhibits antidepressant property in mice (0.3-1 mg/kg i.p.) in vivo. | | in vivo | PDE4B-IN-2 (compound 33; 2 mg/kg; po) has a Cmax of 8.7 μg/mL and an AUC of 52.3 μg h/mL in mice[1].
| | IC 50 | PDE4B: 15 nM (IC50); PDE4D: 1.7 μM (IC50) | | storage | Store at -20°C | | References | [1] Kenji Naganuma, et al. Discovery of selective PDE4B inhibitors. Bioorg Med Chem Lett. 2009 Jun 15;19(12):3174-6. DOI:10.1016/j.bmcl.2009.04.121 |
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