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Shanghai?Medlife?Pharm-Tech?Co.,?Ltd
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021-59167510 18117107507 |
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vip@med-life.cn |
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Product Name:PA-9
CAS:1436004-46-4
Purity:>=99% Package:10mg;1mg;10mM*1mLinDMSO;100mg;50mg;5mg
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| Company Name: |
TargetMol Chemicals Inc.
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15002134094 |
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marketing@targetmol.cn |
| Products Intro: |
Product Name:PA-9
CAS:1436004-46-4
Package:25mg/RMB 10600;100mg/RMB 17500;50mg/RMB 13800
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PHARMEKS Ltd.
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+7 (495) 702-9648 |
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sales@pharmeks.com |
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CAS:1436004-46-4
Package:5μmol Remarks:C17H18N6O2
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| Company Name: |
OTAVA chemicals
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416 305 9979 (Canada) |
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north.america@otavachemicals.com |
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CAS:1436004-46-4
Purity:90%+ Package:5μmol Remarks:C17H18N6O2
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| | N-[2-(1H-imidazol-5-yl)ethyl]-1-(1H-indazol-3-yl)-5-oxopyrrolidine-3-carboxamide Basic information |
| | N-[2-(1H-imidazol-5-yl)ethyl]-1-(1H-indazol-3-yl)-5-oxopyrrolidine-3-carboxamide Chemical Properties |
| Boiling point | 880.0±65.0 °C(Predicted) | | density | 1.440±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO : 250 mg/mL (738.86 mM; Need ultrasonic) | | pka | 13.33±0.40(Predicted) | | form | Solid | | color | White to light yellow |
| | N-[2-(1H-imidazol-5-yl)ethyl]-1-(1H-indazol-3-yl)-5-oxopyrrolidine-3-carboxamide Usage And Synthesis |
| Biological Activity | PA-9 is a pituitary adenylate cyclase-activating polypeptide (PACAP) type I (PAC1) receptor antagonist. PA-9 dose dependently inhibits PACAP-induced cAMP elevation with an IC50 of 5.6 nM. PA-9 can be used for the research of neuropathic and/or inflammatory pain[1].
PA-9 (10 pM to 10 nM; 30 minutes) dose dependently inhibits PACAP-induced (1 nM) CREB phosphorylation in the CHO cells expressing PAC1 receptors[1].
PA-9 (100 pmol; co-injection with PACAP) attenuates the development of PACAP-induced (100 pmol/5 μL; intrathecal injection) aversive responses of mice[1].PA-9 (100 pmol; co-injection with PACAP) significantly blocks the induction of PACAP-induced (100 pmol) mechanical allodynia[1].PA-9 (100 pmol/5 μl; single intrathecal injection alone) does not induce aversive responses and mechanical allodynia of mice[1].PA-9 is well accommodated in the subpocket formed by L80, F81, I83, G91, V92, P107, A112, and C113 of the PAC1 receptor, precipitating in hydrophobic interactions[1]. | | References | [1]. Takasaki I, et al. In Silico Screening Identified Novel Small-molecule Antagonists of PAC1 Receptor. J Pharmacol Exp Ther. 2018 Apr;365(1):1-8. |
| | N-[2-(1H-imidazol-5-yl)ethyl]-1-(1H-indazol-3-yl)-5-oxopyrrolidine-3-carboxamide Preparation Products And Raw materials |
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