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Submit ReviewR 121919 hydrochloride
说明： High affinity CRF1 antagonist; orally bioavailable
化学名： 3-[6-(Dimethylamino)-4-methyl-3-pyridinyl]-2,5-dimethyl-N,N-dipropylpyrazolo[1,5-a]pyrimidin-7-amine hydrochloride
纯度： ≥98% (HPLC)
生物活性 for R 121919 hydrochloride
R 121919 hydrochloride is a high affinity corticotropin releasing factor receptor1 (CRF1) antagonist (Ki = 3.5 nM). Reduces stress-induced elevations of plasma ACTH. Anxiolytic and antidepressant in vivo. Orally bioavailable.
技术数据 for R 121919 hydrochloride
| 分子量 | 416.99 |
| 公式 | C22H32N6.HCl |
| 储存 | Store at +4°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 195055-66-4 |
| PubChem ID | 22029352 |
| InChI Key | LGDDPMVPDGTXMV-UHFFFAOYSA-N |
| Smiles | CCCN(C1=CC(C)=NC2=C(C3=CN=C(N(C)C)C=C3C)C(C)=NN12)CCC.Cl |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for R 121919 hydrochloride
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| ethanol | 41.7 | 100 | |
| DMSO | 4.17 | 10 温和加热 |
制备储备液 for R 121919 hydrochloride
以下数据基于产品分子量 416.99。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.4 mL | 11.99 mL | 23.98 mL |
| 5 mM | 0.48 mL | 2.4 mL | 4.8 mL |
| 10 mM | 0.24 mL | 1.2 mL | 2.4 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.48 mL |
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产品说明书 for R 121919 hydrochloride
参考文献 for R 121919 hydrochloride
参考文献是支持产品生物活性的出版物。
Chen and Grigoriadis (2005) NBI 30775 (R121919), an orally active antagonist of the corticotropin-releasing factor (CRF) type-1 receptor for the treatment of anxiety and depression. Drug Dev.Res. 65 216
Jutkiewicz et al (2005) The effects of CRF antagonists, antalarmin, CP154,526, LWH234, and R121919, in the forced swim test and on swim-induced increases in adrenocorticotropin in rats. Psychopharmacology (Berl). 180 215 PMID: 15696320
Gutman et al (2003) The corticotropin-releasing factor1 receptor antagonist R121919 attenuates the behavioral and endocrine responses to stress. J.Pharmacol.Exp.Ther. 304 874 PMID: 12538845
Heinrichs et al (2002) Brain penetrance, receptor occupancy and antistress in vivo efficacy of a small molecule cortico. releasing factor type I receptor selective antagonist. Neuropsychopharmacology 27 194 PMID: 12093593
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关键词: R 121919 hydrochloride, R 121919 hydrochloride supplier, R121919, HCl, corticotropin, releasing, factor, receptors, 1, CRF1, antagonists, anatgonism, high, affinity, orally, bioavailable, Receptors, 6530, Tocris Bioscience
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
Depression Poster
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.