human m5

VU0238441 is agonist of Muscarinic acetylcholine receptor M5 (human) with EC50 of 2.1μM.

VU 6008667 is a selective negative allosteric modulator (NAM) of the M5 receptor, with IC50 values of 1.2 μM for human M5 and 1.6 μM for rat M5.

PCS1055 dihydrochloride is an effective, selective, and competitive muscarinic M4 receptor antagonist (IC50: 18.1 nM and a Kd: 5.72 nM). PCS1055 dihydrochloride is also a potent AChE inhibitor (IC50 s: 22 nM and 120 nM for electric eel and human AChE, res

ML380 is a highly potent and the first CNS penetrant M5 positive allosteric modulator (PAM).

N-p-Tosyl-Gly-Pro-Lys-pNA is a colorimetric substrate for plasmin.1,2,3Plasmin binds and hydrolyzes N-p-tosyl-Gly-Pro-Lys-pNA to releasep-nitroanilide (pNA), which can be quantified by colorimetric detection at 405 nm as a measure of plasmin activity. 1.Jespersen, J., Gram, J., and Astrup, T.The autodigestion of human plasmin follows a bimolecular mode of reaction subject to product inhibitionThromb. Res.41(3)395-404(1986) 2.Kim, S.H., and Choi, N.S.Electrophoretic analysis of protease inhibitors in fibrin zymographyAnal. Biochem.270(1)179-181(1999) 3.Chen, T., and Rael, E.D.Purification of M5, a fibrinolytic proteinase from Crotalus molossus molossus venom that attacks complementInt. J. Biochem. Cell Biol.29(5)789-799(1997)

DMU-212 is a methylated derivative of resveratrol with antimitotic, anti-proliferative, antioxidant, and apoptosis-promoting activities. It induces mitotic arrest, apoptosis, and activation of ERK1 2 protein and has oral activity[1][2]. DMU-212 (0.3125-40 μM) inhibits the growth of human melanoma cells (A375, MeWo, Bro, M5)[1]. At concentrations of 30-50 μM over 24 hours, it upregulates cell cycle inhibitors, induces apoptosis, and activates ERK in A375 cells[1]. DMU-212 also induces G2 M arrest and apoptosis in cancer cells[1]. In a xenograft model of human ovarian cancer with six-week-old SCID female mice (20-24 g), DMU-212 (50 mg kg, administered orally three times a week for 14 days) inhibits tumor growth[2]. [1]. Vasilis Pericles Androutsopoulos, et al. Activation of ERK1 2 is required for the antimitotic activity of the resveratrol analogue 3,4,5,4'-tetramethoxystilbene (DMU-212) in human melanoma cells. Exp Dermatol. 2015 Aug;24(8):632-4. [2]. Hanna Piotrowska, et al. DMU-212 inhibits tumor growth in xenograft model of human ovarian cancer. Biomed Pharmacother. 2014 May;68(4):397-400.

RO1138452 (CAY10441) is a selective and orally bioavailable antagonist of prostacyclin receptor (pKi: 8.3). It antagonizes the carbaprostacyclin-induced activation of human neuroblastoma adenylate cyclase, blocking cyclic AMP accumulation in a dose-dependent manner. Likewise, it inhibits the binding of tritiated iloprost to rodent neuroblastoma cells with a Ki of about 1.5 nM. At levels between 2-20 mg kg in rats, CAY10441 shows significant analgesic activity in standard antinociceptive assays [1].