PERK-IN-4-d3
PERK-IN-4-d3 is the d3-labeled PERK-IN-4 (HY-137813). PERK-IN-4 is a PERK inhibitor with a human IC50 of 0.3 nM and selectivity relative to other kinases. PERK-IN-4 displays moderate rat blood clearance and pharmacokinetic properties.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- 화학식: C24H16D3F4N5O
- 분자량:472.45
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
제품 설명
IC50 & Target
IC50: 0.3 nM (PERK)[1]
신청
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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Unlabeled CAS 1337531-89-1
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분자량 472.45
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화학식 C24H16D3F4N5O
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SMILES
NC1=C(C2=NC=N1)C(C3=CC=C4C(CCN4C(CC5=CC(C(F)(F)F)=CC(F)=C5)=O)=C3)=CN2C([2H])([2H])[2H]
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocol
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Protocol for Pharmacokinetic Study
Pharmacokinetic studies quantify how an organism handles a drug over time through absorption, distribution, metabolism, and excretion, and the core experimental readout is the concentration-time profile of parent drug and, when relevant, metabolites in biological matrices such as plasma, whole blood, urine, bile, or tissue. Pharmacokinetic analysis links dose, route, exposure, clearance, half-life, distribution, bioavailability, and systemic exposure to drug efficacy and toxicity hypotheses rather than measuring a signaling pathway directly. The literature links pharmacokinetics to drug-development phenotypes by showing that drug metabolism and pharmacokinetics influence compound progression, exposure-response interpretation, safety margins, dosing strategy, and failure risk during discovery and development. DMPK science contributes to compound optimization by integrating physicochemical properties, in vitro metabolism, transporter behavior, in vivo exposure, and pharmacodynamic contex
순도&문서
References
[1]. Axten JM, et al. Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK). Journal of medicinal chemistry. 2012 Aug 23;55(16):7193-207. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)