Rolipram CAS: 61413-54-5
MF: C16H21NO3
MW: 275.35
A selective, cell permeable inhibitor of cAMP-specific phosphodiesterase (PDE4).
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Rolipram (CAS 61413-54-5)

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备用名: SB 95952; ZK 62711
应用； Rolipram is a selective, cell permeable inhibitor of cAMP-specific phosphodiesterase (PDE4)
CAS号码: 61413-54-5
纯度: ≥97%
分子量: 275.35
分子式: C16H21NO3
仅供科研使用。不可用于诊断或治疗。
* 参考分析证明 大量特定数据 (包括水 含量).

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Rolipram is a selective, cell-permeable inhibitor of cAMP-specific PDE (phosphodiesterase) (PDE4, IC50=1 μM). This compound has been shown to inhibit PDE4 activity in human cavernosal tissue, which interrupts the signal transduction pathway of erectile response. Rolipram promotes apoptosis in HL60 cells through a cAMP-independent mechanism and has been shown to enhance neuronal survival. Rolipram is an inhibitor of PDE4A1 and PDE4B.


参考文献

1. Schneider, H.H., et al. 1986. Eur. J. Pharmacol. 127: 105-115. PMID: 3019721
2. Reeves, M.L., et al. 1987. Biochem. J. 241: 535-541. PMID: 3036066
3. Moore, J.B., et al. 1991. Biochem. Pharmacol. 42: 679-683. PMID: 1650219
4. Underwood, D.C., et al. 1994. J. Pharmacol. Exp. Ther. 270: 250-259. PMID: 8035322
5. Zhu, W.H., et al. 1998. Life Sci. 63: 265-274. PMID: 9698035
6. Bivalacqua, T.J., et al. 1999. J. Urol. 162: 1848-1855. PMID: 10524946
7. Sasaki, T., et al. 2007. Stroke. 38: 1597-1605. PMID: 17379823
8. Kaneda, T., et al. 2010. J Smooth Muscle Res. 46: 17-29. PMID: 20383031

用法 :
Following reconstitution, aliquot and freeze (-20°C). DMSO stock solutions are stable for up to 6 months at -20°C.
物理状态 :
Solid
溶解度 :
Soluble in water (0.2 mg/mL ), DMSO (7.3 mg/ml ), ethanol (7 mg/ml warm), DMF (~10 mg/ml ), DMF:PBS (pH 7.2, 1:9) (~0.5 mg/ml ), and acetone (25 mg/ml).
保存 :
Store at 4° C
熔点 :
184.12° C (Predicted)
沸点 :
~472.7° C at 760 mmHg (Predicted)
密度 :
~1.2 g/cm3 (Predicted)
折射率 :
n20D 1.55
IC50 :
cAMP-specific phosphodiesterase (PDE4): IC50 = 1 µM; C5a-stimulated LTC4 synthesis: IC50 = 200 nM (eosinophils); lipopolysaccharide-induced TNF synthesis: IC50 = 360 nM (monocytes); Phosphodiesterase 4A: IC50 = 4 nM (mouse); Phosphodiesterase 4B: IC50 = 34 nM (human); Phosphodiesterase 4D: IC50 = 25 nM (human); Phosphodiesterase 4C: IC50 = 25 nM (human)
Ki 数据 :
Phosphodiesterase 4A: Ki= 0.0023 nM (Rattus norvegicus); Phosphodiesterase 4D: Ki= 1.6 nM (human); Phosphodiesterase 4B: Ki= 3.8 nM (human); Phosphodiesterase 4C: Ki= 0.0023 nM (Rattus norvegicus)
仅供科研使用。不可用于诊断或治疗。
德国水公害等级 :
3
RTECS :
UY5749237
PubChem CID :
5092
默克索引 :
14: 8251
MDL 号码 :
MFCD00270906
EC号码 :
262-771-1
SMILES :
COC1=C(C=C(C=C1)C2CC(=O)NC2)OC3CCCC3

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引用1 - 10 的 17

PMID: # 25931510  Reddy, GR.|Subramanian, H.|Birk, A.|Milde, M.|Nikolaev, VO.|Bünemann, M.| et al. 2015. FASEB J. 29: 3458-71.

PMID: # 26416856  Euba, B. et al. 2015. Antimicrob. Agents Chemother. 59: 7581-92.

PMID: # 18372231  Levallet, G. et al. 2008. J. Endocrinol. 197: 45-54.

PMID: # 18641359  Hervé, R et al. 2008. J. Immunology. 181: 2196-2202.

PMID: # 16968783  Sohara, E. et al. 2006. Proc. Natl. Acad. Sci. USA. 103(38): 14217-14222.

PMID: # 16177794  Dodge-Kafka KL et al. 2005. Nature. 437(7058): 574-578.

PMID: # 16192372  Patwardhan, AM. et al. 2005. J Neurosci. 25(39): 8825-8832.

PMID: # 16083514  Yao, PL. et al. 2005. Respir. Res. 6: -.

PMID: # 15930146  Cheng, J. et al. 2005. Am. J. Physiol., Cell Physiol. 289: C959-C970.

PMID: # 11934820  Nagakura, A. et al. 2002. Br. J. Pharmacol. 135: 1783-1793.

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