at-130

AT-130 是一种苯基丙烯酰胺衍生物，是乙型肝炎病毒复制的非核苷抑制剂。它抑制病毒 DNA 的合成，EC50为 0.13 μM。

S-Nitrosothiols (RSNOs) are a class of molecules that function as exogenous and endogenous nitric oxide (NO) donors. RSNOs found in vivo include proteins such as S-nitrosohemoglobin and S-nitrosoalbumin, as well as low molecular weight species such as S-nitrosoglutathione (GSNO) and S-nitrosocysteine (CysNO). CAY10565 is a member of a new class of S-nitrosothiol species that act as NO donors under acidic conditions. It decomposes with a half-life of 130 minutes in 0.1 M phosphate buffer, pH 5.0, at 37°C and relaxes phenylephrine-constricted rat aortic strips 71% and 44% at pH 6.0 and 7.4, respectively.

15(R)-Pinane thromboxane A2 is the (R)-epimer of pinane thromboxane A2 . 15(R)-PTA2 does not inhibit collagen-induced platelet aggregation (IC50s = 120-130 μM). It does not affect gastric tone in isolated rat gastric fundus when used at concentrations of 0.5 or 1.5 μg ml and is less effective than PTA2 at inhibiting prostaglandin-induced contraction of isolated rat stomach muscle.

Streptazolin is a fungal metabolite originally isolated from S. viridochromogenes. It increases NF-κB activity when used at concentrations ranging from 60 to 130 μg ml, at least in part, via PI3K signaling. Streptazolin enhances TNF-α secretion induced by LPS and enhances IL-8 secretion when used alone or in combination with LPS in THP-1 Blue cells.

TLQP-21 TFA, a VGF-derived peptide endowed of endocrine and extraendocrine properties, is a potent G-protein-coupled receptor complement-3a receptor1 (C3aR1) agonist (EC50: mouse TLQP-21=10.3 μM; human TLQP-21=68.8μM). TLQP-21 TFA activates C3aR1 to induce an increase of intracellular Ca2+. TLQP-21 TFA is used for the research in regulation of nociception and other relevant physiologic functions[1][2]. TLQP-21 TFA is a peptide of 21 amino acids. At a dose of 3 μM TLQP-21 induces up to ~69% of the corresponding contraction promoted by acetylcholine[1][2]. [1]. Elena Bresciani , et al. TLQP-21, A VGF-Derived Peptide Endowed of Endocrine and Extraendocrine Properties: Focus on In Vitro Calcium Signaling. Int J Mol Sci. 2019 Dec 24;21(1):130. [2]. Cheryl Cero, et al. The TLQP-21 Peptide Activates the G-protein-coupled Receptor C3aR1 via a Folding-Upon-Binding Mechanism. ructure. 2014 Dec 2;22(12):1744-1753.

Benzomalvin C is a weak antagonist of the neurokinin-1 (NK1) receptor inhibiting binding of substance P by 46% when used at 100 μg ml in vitro. It is also a weak inhibitor of indolamine 2,3-dioxygenase (IDO) with an IC50 value of 130 μM for recombinant IDO. It was isolated from Penicillium and contains an epoxide group at C-19 and C-20, which is not present in benzomalvins A, B, or E.

PLX647 dihydrochloride is a potent and selective dual inhibitor of FMS and KIT kinases, with IC50 values of 28 nM and 16 nM, respectively. At a concentration of 1 μM, PLX647 dihydrochloride demonstrates superior selectivity against a wide range of 400 kinases, except FLT3 and KDR, where IC50 values are 91 nM and 130 nM, respectively. This orally active compound holds great potential for targeted kinase inhibition.

Zicronapine (Lu 31-130) fumarate 是抗精神病药，主要通过拮抗多巴胺D1 D2受体和5-HT2A受体发挥作用，在动物模型中显示出显著的前认知效果，展现出治疗多种神经和精神疾病的可能性。

ZXH-4-130 TFA为高效、选择性CRBN降解剂，属于CRBN-VHL类(hetero-PROTAC)化合物。在MM1.S细胞中，10 nM ZXH-4-130 TFA可诱导约80%的CRBN降解。

PGD97 是一种选择性环肽抑制剂，针对 CAL CFTR 相互作用。其脱硫环化形式对 CAL PDZ 域的 KD 值为 6 nM。相较于 NHERF1 2 PDZ 域，PGD97 (脱硫环化形式) 的选择性至少高出 130 倍。PGD97 能够在细胞膜上稳定 F508del-CFTR，改善维持肺部正常液体平衡所需的 CFTR 功能。PGD97 可应用于囊性纤维化研究。