Parstatin(human), a cell-penetrating PAR-1 thrombin receptor agonist peptide, is a potent inhibitor of angiogenesis[1][2].
vMIP-II (1-21) is a CXCR4 antagonist. vMIP-II has broad-spectrum interaction with CC and CXC chemokine receptors. vMIP-II (1-21) binds with CXCR4 with an IC50 value of 190 nM for competing with CXCR4 binding of 125I-SDF-1R[1].
KRAS G12C inhibitor 47 (compound 8-1-1) is a potent KRAS G12C inhibitor with an IC50 of 0.172 µM. KRAS G12C inhibitor 47 shows p-ERK inhibition activities with IC50s of 0.046, 69.8 µM in MIA PaCA-2, A549 cells, respectively. KRAS G12C inhibitor 47 has the potential for the research of pancreatic, colorectal, and lung cancers[1].
Auriculasin is a nature product isolated from Limonium leptophyllum. Auriculasin has activity toward cannabinoid receptor type 1 (CB1) with an IC50 value of 8.92 µM[1].
WAY-100635 is a potent and selective 5-HT1A Receptor antagonist with a pIC50 of 8.87, an apparent pA2 of 9.71.
Suntinorexton, a heterocyclic compound, is an orexin type 2 receptor agonist extracted from patent WO2019027058A1, page 288[1].
ZD 7155 hydrochloride is an angiotensin II receptor type 1 (AT1 receptor) antagonist.
CAY10789 (compound 6) is a potent CysLT1R (cysteinyl leukotriene receptor 1) antagonist (IC50=2.80 μM) and GPBAR1 (G-protein-coupled bile acid receptor 1) agonist (EC50=3 μM). CAY10789 significantly reduces the adhesion of U937 cells to HAEC, reduces the expression of TNF-α. CAY10789 shows very promising metabolic stability and excellent pharmacokinetics. CAY10789 can be used for the research of colitis, metabolic syndromes, and other GPBAR1/CysLT1R-related diseases[1].
HY-101653 is a drug with multiple CNS targets, and inhibits acetylcholinesterase (AChE) with Ki of 69 μM; also active against muscarinic M1 and M2 receptors, serotonin 5HT4 receptors, and imidazole I2 receptors.
SC-41930 is a orally active eukotriene-B4 receptor antagonist. SC-41930 alleviates inflammation in guinea pig acetic acid-induced colonic inflammation model[1].
Zuclopenthixol-d4((Z)-Clopenthixol-d4) succinate salt is the deuterium labeled Zuclopenthixol. Zuclopenthixol is a thioxanthene derivative which acts as a mixed dopamine D1/D2 receptor antagonist[1][2].
Pridopidine, a dopamine (DA) stabilizer, acts as a low affinity dopamine D2 receptor (D2R) antagonist. Pridopidine exerts high affinity towards sigma 1 receptor (S1R) with Ki between 70 and 80 nM, which is ~100× higher than its affinity toward D2R.
(R)-Casopitant ((R)-GW679769) is the isomer of Casopitant (HY-14405). Casopitant is a NK(1)-receptor antagonist. Casopitant can be used for the research of chemotherapy-induced nausea and vomiting[1][2].
Glucagon receptor antagonists-2 is a highly potent glucagon receptor antagonist.
2-(3-Trifluoromethylphenyl)glycine hydrochloride is a precursor of substituted 2-acetamido-5-aryl-l, 2,4-triazolones. Substituted 2-acetamido-5-aryl-l, 2,4-triazolones are dual V1a/V2 receptor antagonists and can be used in cardiovascular disease research[1].
Gallamine Triethiodide is a synthetic nondepolarizing blocking drug.Target: mAChRGallamine triethiodide is a non-depolarising muscle relaxant. It acts by combining with the cholinergic receptor sites in muscle and competitively blocking the transmitter action of acetylcholine. Gallamine triethiodide has a parasympatholytic effect on the cardiac vagus nerve which causes tachycardia and occasionally hypertension. Very high doses cause histamine release. Gallamine triethiodide is commonly used to stabilize muscle contractions during surgical procedures. From Wikipedia.
KRAS G12C inhibitor 19 is a potent inhibitor of KRAS G12C. KRAS G12C inhibitor 19 significantly inhibits tumor growth (extracted from patent WO2021118877A1)[1].
Pitolisant is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM).
Ivabradine D3 Hydrochloride is the deuterium labeled Ivabradine hydrochloride. Ivabradine hydrochloride is a new If inhibitor with IC50 of 2.9 μM, and used as a pure heart rate lowering agent.
(R)-3-O-Methyldopa-d3 hydrochloride is a deuterium labeled (R)-3-O-Methyldopa, and (R)-3-O-Methyldopa is an R-enantiomer of 3-O-Methyldopa. 3-O-Methyldopa is a metabolite of L-DOPA which is formed by catechol-O-methyltransferase (COMT). 3-O-Methyldopa competitively inhibits the pharmacodynamics of L-DOPA and dopamine[1][2].
Clomipramine HCl is a serotonin transporter (SERT), norepinephrine transporter (NET) dopamine transporter (DAT) blocker with Ki of 0.14, 54 and 3 nM, respectively. Target: 5-HT ReceptorClomipramine hydrochloride (Anafranil) is a hydrochloride salt of clomipramine which is a serotonin transporter (SERT), norepinephrine transporter (NET) dopamine transporter (DAT) blocker with Ki of 0.14, 54 and 3 nM, respectively. Clomipramine hydrochloride (Anafranil) is a tricyclic antidepressant. Clomipramine hydrochloride (Anafranil) is a norepinephrine-reuptake inhibitor and is an antiobsessional drug. Clomipramine hydrochloride (Anafranil) is an antagonist/inverse agonist at the following receptors: D2 receptor (Ki = 162 nM), D3 receptor (Ki = 30 nM), α1-adrenergic receptor (Ki = 3.2 nM), α2-adrenergic receptor (Ki = 525 nM), H1 receptor (Ki = 31 nM), mACh receptors (Ki = 37 nM), 5-HT2A receptor (Ki = 36 nM), 5-HT2C receptor (Ki = 65 nM), 5-HT3 receptor (Ki = 85 nM), 5-HT6 receptor (Ki = 54 nM), 5-HT7 receptor (Ki = 127 nM), D1 receptor (Ki = 219 nM) [1-3].
NK3R-IN-1 (compound 16x), a imidazolepiperazine derivative, is an orally active Neurokinin Receptor NK3R inhibitor. NK3R-IN-1 decreases blood luteinizing hormone levels in ovariectomy (OVX) model[1].
CGP-42112(CGP-42112A) is a potent Angiotensin-II subtype 2 receptor(AT2 R) agonist.IC50 value:Target: AT2 R agonistin vitro: CGP42112 (>==1 nM) significantly inhibited cGMP production from the basal value. CGP42112 (>==1 nM) significantly inhibited TH-enzyme activity from the basal value. These inhibitory effects of CGP42112 on TH-enzyme activity and-cGMP production were abolished by PD123319 (AT(2)-R antagonist) while CV-11974 (AT(1)-R antagonist) was ineffective [1]. [125I]CGP 42112 bound selectively to the AT2 angiotensin II receptor subtype. [125I]CGP 42112 bound with higher affinity in the brain than in the adrenal. beta-Mercaptoethanol enhanced [125I]CGP 42112 binding in the brain, but did not alter its binding in the adrenal [2]. [125I]CGP 42112 bound with high affinity (Kd = 0.07-0.3 nM, depending on the area studied). [125I]CGP 42112 binding was selective for AT2 receptors, as determined by lack of competition with the AT1 ligand losartan, and competition by the AT2 ligands PD 123177 and unlabeled CGP 42112 and the non-selective peptides Ang II and angiotensin III (Ang III) [4].in vivo: Intravenous infusions of CGP 42112 (0.1 and 1 mg kg-1 min-1) and PD 123319 (0.36 and 1 mg kg-1 min-1) shifted the upper limit of CBF autoregulation toward higher blood pressures without affecting baseline CBF [3].
(R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
Bisoprolol is a potent, selective and orally active β1-adrenergic receptor blocker. Bisoprolol has little activity on β2-receptor and has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research[1][2].
Nemorexant is a potent orexin receptor antagonist extracted from patent WO2015083094A1, compound example 7, has IC50s of 2 nM and 3 nM for Ox1 receptor and Ox2 receptor, respectively.
Bromodiphenhydramine (Ambodryl) is a potent antihistamine with antimicrobial property. Bromodiphenhydramine inhibits a large number of Gram negative and Gram positive bacteria. Bromodiphenhydramine can be used for cutaneous allergies research[1][2][3].
Nyasol ((-)-Nyasol) is an active compound that has antifungal, antibacterial, antileishmanial, hyaluronidase inhibition activities. Nyasol inhibits LTB4 binding to human neutrophils. Nyasol suppresses neuroinflammatory response through the inhibition of I-κB degradation in LPS (HY-D1056)-stimulated BV-2 microglial cells[1][2].
HEMADO is a potent and selective adenosine A3 receptor agonist with a Ki of 1.1 nM at the human A3 subtype[1].
OX2R-IN-1 is a low cytotoxicity profile OX2R-IN-1 antagonist (a potential OX2R binder) with an IC50 value of 484 μM. OX2R-IN-1 can cross the BBB into the brain with a short half-life[1].