N-[2-(1H-imidazol-5-yl)ethyl]-1-(1H-indazol-3-yl)-5-oxopyrrolidine-3-carboxamide manufacturers
- PA-9
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- $1520.00
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2026-04-20
- CAS:1436004-46-4
- Purity:
- Supply Ability: 10g
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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 |
| Uses | 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]. | | 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]. | | in vivo | 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].
| Animal Model: | Male ddY mice (6 weeks old at the start of experiments; intrathecal injection 100 pmol/5 μL PACAP)[1] | | Dosage: | intrathecal injection, co-injection with PACAP. | | Administration: | 100 pmol/5 μL
| | Result: | Attenuated the development of PACAP-induced aversive responses.
Blocked the induction of PACAP-induced mechanical allodynia.
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| | IC 50 | PAC1 receptor | | 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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