by-217

Roflumilast (APTA 2217) 是一种口服的长效 4 型磷酸二酯酶抑制剂 (PDE4)，具有抗炎和潜在的抗肿瘤活性，作用于PDE4A1，PDEA4，PDEB1和PDEB2，IC50分别为 0.7，0.9，0.7 和 0.2 nM。

Biotin (S)-sulfoxide is an inactive metabolite of the coenzyme biotin .1,2It has also been found inE. coliand is reduced by the biotin sulfoxide reduction system as a source of biotin.3 1.Denkel, L.A., Rhen, M., and Bange, F.-C.Biotin sulfoxide reductase contributes to oxidative stress tolerance and virulence in Salmonella enterica serovar TyphimuriumMicrobiology (Reading)159(Pt 7)1447-1458(2013) 2.Carling, R.S., and Turner, C.Methods for assessment of biotin (Vitamin B7)Laboratory assessment of vitamin status193-217(2019) 3.del Campillo-Campbell, A., Dykhuizen, D., and Clearly, P.P.Enzymic reduction of d-biotin d-sulfoxide to d-biotinMethods Enzymol.62379-385(1979)

NGB 2904 是一种具有口服活性的、选择性的多巴胺(DA) D3受体拮抗剂，可用于具可卡因成瘾。

OH-Chol is a cationic cholesterol derivative.1 OH-Chol, as a component of lipoplexes with DOPE , has been used for siRNA delivery and gene silencing in MCF-7 cells, as well as in mice via intravenous injection, resulting in lipoplex accumulation in the liver. It has also been used in cationic nanoparticles in combination with Tween 80 to transfect pDNA and siRNA into PC3 mouse xenografts via intratumoral injection and with Tween 80 and folate-PEG2000-DSPE in a KB mouse xenograft model for intratumoral gene delivery.2References1. Hattori, Y., Nakamura, M., Takeuchi, N., et al. Effect of cationic lipid in cationic liposomes on siRNA delivery into the lung by intravenous injection of cationic lipoplex. J. Drug. Target 27(2), 217-227 (2019).2. Hattori, Y. Development of non-viral vector for cancer gene therapy. Yakugaku Zasshi 130(7), 917-923 (2010). OH-Chol is a cationic cholesterol derivative.1 OH-Chol, as a component of lipoplexes with DOPE , has been used for siRNA delivery and gene silencing in MCF-7 cells, as well as in mice via intravenous injection, resulting in lipoplex accumulation in the liver. It has also been used in cationic nanoparticles in combination with Tween 80 to transfect pDNA and siRNA into PC3 mouse xenografts via intratumoral injection and with Tween 80 and folate-PEG2000-DSPE in a KB mouse xenograft model for intratumoral gene delivery.2 References1. Hattori, Y., Nakamura, M., Takeuchi, N., et al. Effect of cationic lipid in cationic liposomes on siRNA delivery into the lung by intravenous injection of cationic lipoplex. J. Drug. Target 27(2), 217-227 (2019).2. Hattori, Y. Development of non-viral vector for cancer gene therapy. Yakugaku Zasshi 130(7), 917-923 (2010).

Methoctramine is a selective antagonist of M2 muscarinic acetylcholine receptors (IC50 = 6.1 nM in CHO-K1 cell membranes).[1] It is selective for M2 over M1, M3, M4, and M5 receptors (IC50s = 92, 770, 260, and 217 nM, respectively). In vitro, methoctramine inhibits acetylcholine-induced reductions in isolated guinea pig tracheal tube contractions when used at a concentration of 1 μM.[2] In vivo, methoctramine inhibits bradycardia and bronchoconstriction induced by acetylcholinein guinea pigs with ED50 values of 38 and 81 nmol kg, respectively. In a rat model of spinal cord injury, methoctramine suppresses bladder overactivity induced by the non-selective muscarinic acetylcholine receptor agonist oxotremorine M.[3]

Gp100:209-217 由 HLA-A2 表达的 gp100 衍生的人类 CTL 表位，是一种含有 8 种氨基酸的多肽，且为有效的 TGF-β 抑制剂，可阻断 TGF-β 信号通路。