生物活性 | PACAP (6-38), human, ovine, rat TFA is a potentPACAP receptorantagonist withIC50s of 30, 600, and 40 nM forPACAP type I receptor,PACAP type II receptor VIP1, andPACAP type II receptor VIP2, respectively. | ||||||||||||||||
IC50& Target | IC50: 30 nM (PACAP type I receptor), 600 nM (PACAP type II receptor VIP1), 40 nM (PACAP type II receptor VIP2)[1] | ||||||||||||||||
体外研究 (In Vitro) | An increase of dopamine (DA) content by HPLC analysis and/or cell proliferation identified by MTT assay by Dexamethasone (DEX) is also observed which can be inhibited by PACAP (6-38) at concentration sufficient to block PACAP type 1 (PAC1) receptor. Pretreatment with PAC1 receptor antagonist PACAP (6-38) at 0.1 or 1 μM for 2 h significantly blocks this increase of DA content by 1 μM DEX. The MTT assay shows that DEX increases cell proliferation. Moreover, this action is also inhibited by the pre-incubation of PACAP (6-38). PACAP (6-38) at 1μM shows no effect on DA content and cell proliferation for 24 h. However, PACAP (6-38) at 0.3 μM has been mentioned to reduce the spontaneous tyrosine hydroxylase (TH) accumulation in differentiated retinal cultured cells for 5 days[2]. | ||||||||||||||||
体内研究 (In Vivo) | Intravesical administration of the PAC1 receptor antagonist, PACAP (6-38), significantly increases intercontraction interval (2.0-fold) and void volume (2.5-fold) in NGF-OE mice. Intravesical instillation of PACAP (6-38) also decreases baseline bladder pressure in NGF-OE mice. Intravesical administration of PACAP (6-38) (300 nM) significantly (p≤0.01) reduces pelvic sensitivity in NGF-OE mice but is without effect in WT mice[3]. | ||||||||||||||||
分子量 | 4138.76 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C184H301N56FO47S | ||||||||||||||||
Sequence | Phe-Thr-Asp-Ser-Tyr-Ser-Arg-Tyr-Arg-Lys-Gln-Met-Ala-Val-Lys-Lys-Tyr-Leu-Ala-Ala-Val-Leu-Gly-Lys-Arg-Tyr-Lys-Gln-Arg-Val-Lys-Asn-Lys-NH2 | ||||||||||||||||
Sequence Shortening | FTDSYSRYRKQMAVKKYLAAVLGKRYKQRVKNK-NH2 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | Sealed storage, away from moisture
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) | ||||||||||||||||
溶解性数据 | In Vitro: DMSO : 100 mg/mL(24.16 mM;Need ultrasonic) H2O : 50 mg/mL(12.08 mM;Need ultrasonic) 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
*以上所有助溶剂都可在本网站选购。 |
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