RS-127445 is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with a pKi of 9.5. RS-127445 shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites[1].
AdipoRon hydrochloride is an orally active and specific AdipoR agonist, binding to AdipoR1 and AdipoR2, with Kds of 1.8 and 3.1 μM, respectively.
C-Type Natriuretic Peptide (CNP) (1-22), human is the 1-22 fragment of C-Type Natriuretic Peptide. C-type natriuretic peptide is natriuretic peptide family peptide that is involved in the maintenance of electrolyte-fluid balance and vascular tone.
GS-6201 (CVT-6883) is a selective adenosine A2B receptor antagonist. GS-6201 displays high affinity and selectivity for the human adenosine A2B receptors (Ki=22 nM)[1]. GS-6201 reduces caspase-1 activity in the heart, and attenuates cardiac remodeling after acute myocardial infarction (AMI) in the mouse[2]. GS-62013 attenuates the airway reactivity induced by NECA, AMP, or allergen in sensitized mice[3].
HOKU-81, a new bronchodilator, is one of the metabolites of tulobuterol. IC50 Value: Target: Adrenergic ReceptorEffects of HOKU-81 on isolated trachea and atria of guinea pigs were compared with those of various bronchodilators. HOKU-81 appears to be a potent and selective beta 2-stimulant with a slight inotropic action. HOKU-81 was approximately 8 times more potent than tulobuterol, approximately twice as potent as salbutamol, and approximately as potent as isoprenaline in relaxing effect on the isolated tracheal smooth muscle preparation of guinea pigs. This effect of HOKU-81 seems to be due to direct action on the adrenergic beta-receptor.
Levalbuterol ((R)-Albuterol; (R)-Salbutamol) is a short-acting β2-adrenergic receptor agonist and the active (R)-enantiomer of Salbutamol. Levalbuterol is a more potent bronchodilator than Salbutamol and has the potential for the treatment of COPD[1].
LY379268 is a potent, selective and brain-penetrant mGlu2/3R agonist with EC50 values of 2.69 nM (mGlu2) and 4.48 nM (mGlu3). LY379268 has no activity on human mGlu 1a, 4a, 5a or 7a receptors. LY379268 has antioxidant and neuroprotective effects[1][2].
Fesoterodine Fumarate is an antimuscarinic agent and is rapidly de-esterified to its active metabolite 5-hydroxymethyl tolterodine that is a muscarinic receptor antagonist.IC50 value:Target: mAChRFesoterodine has the advantage of allowing more flexible dosage than other muscarinic antagonists. Its tolerability and side effects are similar to other muscarinic antagonists and as a new drug seems unlikely to make great changes in practices of treatment for overactive bladder.
AP521 is an agonist of human 5-HT1A receptor with an IC50 of 94 nM.
Bamirastine inhibits ligand binding to recombinant human histamine H1 receptors (rhH1R) with an IC50 value of 17.3 nM.
Meranzin is an absorbed bioactive compound from the Traditional Chinese Medicine (TCM) Chaihu-Shugan-San (CSS). Meranzin, isolated from leaves of Murraya exotica L., regulates the shared alpha 2-adrenoceptor and involves the AMPA-ERK1/2–BDNF signaling pathway. Meranzin has the potential for the prevention of the comorbidity of atherosclerosis and depression[1][2].
Fenoldopam(SKF 82526) is a drug and synthetic benzazepine derivative which acts as a selective D1 receptor partial agonist.Target: D1 ReceptorFenoldopam is a selective dopamine-1 (DA1) agonist with natriuretic/diuretic properties. Fenoldopam stimulated cAMP accumulation in LLC-PK1 cells in a dose-dependent manner, an effect which could be blocked by the DA1-selective antagonist Sch 23390. Although fenoldopam was more potent than DA (EC50 55.5 +/- 7.75 nM vs. 1.65 +/- 0.64 microM) in stimulating cAMP accumulation in LLC-PK1 cells, the maximum stimulation obtained by fenoldopam was only 37% of the maximum stimulation obtained by DA(Emax 13.0 +/- 2.95 pmol/mg of protein vs. 35.6 +/- 10.19 pmol/mg of protein) [1]. Fenoldopam is a selective dopamine1 (DA1) receptor agonist. Most of the DA1 receptor agonist activity of fenoldopam resides in the R-enantiomer, which also shows weaker alpha 2-adrenoceptor antagonist activity Fenoldopam produces vasodilation in vascular beds that are rich in vascular DA1 receptors [2].
Loteprednol Etabonate is an anti-inflammatory corticosteroid used in optometry and ophthalmology.IC50 Value:Target: Glucocorticoid Receptorin vitro:in vivo: Intravenous administration of loteprednol etabonate (5 mg/kg) to dogs revealed a terminal half-life of 2.8 h, a volume of distribution of 3.7 L/kg, and a total body clearance of 0.9 L/h/kg. Intact loteprednol etabonate was not detectable in the urine. After oral administration of the drug (5 mg/kg) to dogs, only metabolites, but no intact drug, were found in the plasma, an indication for a high first-pass effect. A pronounced binding of the drug to plasma protein (> 90%) and a high erythrocyte-buffer partition coefficient of 7.8 were determined in vitro.
Cariprazine D8 (RGH-188 D8) is a deuterium labeled Cariprazine. Cariprazine is a novel antipsychotic drug candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM).
MRE3008F20 is a highly potent and selective antagonistic of adenosine A3 receptor (AA3R), inhibits agonist-induced cAMP elevation in resting T lymphocytes with an IC50 of 5 nM[1].
HT-2157 (SNAP 37889) is a selective, high-affinity, competitive antagonists of galanin-3 receptor (Gal3).
Big Endothelin-1 (1-38), human is the precursor of endothelin-1. Endothelin-1 (ET-1) is a potent vasopressor peptide[1].
[Ala1,3,11,15]-Endothelin (53-63) is an ETB agonist. [Ala1,3,11,15]-Endothelin (53-63) has selectivity for ETB with IC50 values range from 0.33 nM to 0.61 nM. [Ala1,3,11,15]-Endothelin (53-63) can be used for the research of vasoconstriction[1][2].
Rhosin is a specific Rho inhibitor; binds to WT RhoA with an affinity ~0.4 uM Kd; does not interfere with the binding of Cdc42 or Rac1.IC50 value: 0.4 uM(binding Kd) [1]Target: RhoA inhibitorRhosin is specific to the interaction between RhoA and its GEFs including LARG, DBL, LBC, p115 RhoGEF or PDZ RhoGEF and does not interfere with the binding of Cdc42 or Rac1 to their respective GEFs. Rhosin showed a dose-dependent inhibition of endogenous RhoA activity and cell growth of MCF7 cells. Rhosin dose-dependently reduced RhoA and p-MLC1 activities of MCF7 cell-derived mammospheres with an EC50 ~30-50μM, and caused decreased size and reduced number of mammospheres in MCF7 cells [1]. Y16 works synergistically with Rhosin/G04, a Rho GTPase activation site inhibitor, in inhibiting LARG-RhoA interaction, RhoA activation, and RhoA-mediated signaling functions [2].
KRAS G12C inhibitor 13 is a KRAS G12C inhibitor extracted from patent WO2018143315A1, compound 30[1].
Hemopressin(rat) is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin(rat) exerts antinociceptive action in inflammatory pain models[1][2].