rp 8

Rp-8-CPT-cAMP is a structural combination of the lipophilic and non-hydrolyzable cAMP analogs, 8-CPT-cyclic AMP and Rp-cyclic AMPS .[1] It functions as a site-selective inhibitor of protein kinase A (PKA) type I and II, with preference towards site A of type I and site B of type II.2 By occupying cAMP binding sites at the regulatory subunit of PKA, Rp-8-CPT-cAMP prevents the kinase holoenzyme from dissociative activation.[2],[3]

Rp-8-CPT-cAMPS is a powerful and competitive antagonist of cAMP-induced activation of cAMP-dependent protein kinase (PKA) I and II. Acting as a potent cAMP analog, Rp-8-CPT-cAMPS exhibits a preference for site A of RI over site A of RII. Additionally, it favors site B of RII over site B of RI. This compound effectively inhibits cAMP-dependent PKA activation and demonstrates selectivity in binding to specific sites within the protein kinase.

Rp-8-pCPT-cGMPS 是一种具有高脂溶性的 cGMP 依赖性蛋白激酶 (PKG) 竞争性抑制剂,其抑制常数 (Ki) 为 0.5 μM.此化合物能轻易穿透细胞膜,于细胞内聚集达到有效浓度,从而抑制 cGMP 依赖性蛋白激酶的活性.Rp-8-pCPT-cGMPS 常用于探究血小板中 cGMP 依赖性蛋白激酶的活性与功能.

Rp-8-Br-cAMPS 作为PKA的抑制剂，通过与调节亚基的cAMP结合位点相结合，避免了PKA的解离和激活。此外，Rp-8-Br-cAMPS在逆转录病毒感染的小鼠模型中能够增强免疫功能。

cGMP-dependent protein kinase (PKG) inhibitor

Rp-8-bromo-Cyclic AMPS (Rp-8-bromo-cAMPS) is a cell-permeable cAMP analog that combines an exocyclic sulfur substitution in the equatorial position of the cyclophosphate ring with a bromine substitution in the adenine base of cAMP. It acts as an antagonist of cAMP-dependent protein kinases (PKAs) and is resistant to hydrolysis by cyclic nucleotide phosphodiesterases. Rp-8-bromo-cAMPS more effectively antagonizes cAMP-dependent activation of purified PKA type I from rabbit muscle than PKA type II from bovine heart.

Rp-8-Br-cGMPS sodium salt不仅是有效的Ca2+-ATPase激活剂,而且还能作为杆状CNG通道的激动剂和PKG的抑制剂.这种化合物通过激活Ca2+-ATP酶,进而促进细胞内Ca2+的去除,从而降低胞质中的Ca2+水平.

CGRP 8-37 (rat) 是 CGRP receptor 拮抗剂，是一种可作用于大鼠的 CGRP片段，具有潜在的抗伤害作用，可诱导动脉松弛。

[D-Trp8]-γ-MSH acetate(321351-81-9 free base) 是选择性黑皮质素 3 (MC3) 受体激动剂（对人 MC3、MC5 和 MC4 受体的 IC50 值分别为 6.7、340 和 600 nM）。显示有抗炎功效。

Calcitonin Gene Related Peptide (CGRP) (83-119), rat is a 37 amino acid calcitonin family of neuropeptide, acts through calcitonin receptor-like receptor.

13-Oxopodocarp-8(14)-en-18-oic acid 是一种天然产物，可用于生命科学领域的相关研究。其产品编号为 TN2619，CAS号为 63976-69-2。

[D-Trp8,Tyr11] Somatostatin是一种somatostatin的类似物，后者是一种调节多种身体机能的激素。在该化合物中，DTrp8残基的加入可以提高其稳定性。

CGRP (83-119), rat TFA (Calcitonin Gene Related Peptide(83-119), rat TFA) 是一种由 37 个氨基酸组成的神经肽降钙素家族，通过降钙素受体样受体起作用。

Tyr-(D-Dab4,Arg5,D-Trp8)-cyclo-Somatostatin-14 (4-11)，一种生长抑素激动剂，用于癌症研究。

Agouti-related Protein (AGRP) (83-132) Amide (human)，一种AGRP的片段，主要在下丘脑弓状核中表达。该化合物主要通过作为黑皮质素-4受体(MC4R)的反向激动剂来增加食物摄入。

[D-Trp8]-γ-MSH is a selective melanocortin 3 (MC3) receptor agonist (IC50 values are 6.7, 340 and 600 nM for human MC3, MC5 and MC4 receptors respectively). [D-Trp8]-γ-MSH displays anti-inflammatory efficacy.

Rat CGRP-(8-37) (VTHRLAGLLSRSGGVVKDNFVPTNVGSEAF) is a highly selective CGRP receptor antagonist

(D-Trp8,D-Cys14)-Somatostatin-14 为一种生长抑素合成类似物，主要用于代谢相关疾病研究。

HCGRP-(8-37) acetate 是一种人降钙素基因相关肽 (hCGRP) 片段醋酸盐，也是 CGRP 受体的拮抗剂。

[D-Trp8] Somatostatin-14为一种十四肽生长抑素类似物，其活性优于天然Somatostatin。

7,15-Dihydroxypodocarp-8(14)-en-13-one 是一种天然产物，可用于生命科学领域的相关研究。其产品编号为 TN3206，CAS号为 262355-96-4。

[D-Trp8]-γ-MSH TFA 是一种有效的、选择性的黑皮质素3 (MC3)受体激动剂，在 CHO 细胞中，抑制 hMC3，hMC4和 hMC5的 IC50值分别为 6.7 nM，600 nM 和 340 nM。[D-Trp8]-γ-MSH TFA 显示出对多种炎症性疾病(如类风湿关节炎和结肠炎)的保护作用。

(D-Phe5,Cys6,11,N-Me-D-Trp8)-Somatostatin-14 (5-12) amide (Compound 4) 是一种生长抑素类似物，对 SSTR5、SSTR3、SSTR2、SSTR1和 SSTR4的Kd 分别为 0.61、11.05、23.5、1200 和 >1000 nM。

RP-72540 is a cholecystokinin B receptor antagonist. RP 72540 showed selectivity factors in express of 200 for CCKA versus CCKB receptors and also had high affinity for gastrin binding sites in the stomach. Administration of RP-72540 resulted in a dose-de