MTPG is a potent mGluR2 and mGluR3 antagonist. MTPG can block the induction of brain ischemic tolerance induced by cerebral ischemic preconditioning. MTPG also significantly attenuates the inhibitory effect of L-CCG-1 on the KCl-evoked dopamine release[1].
AZP-531 is an analogue of unacylated ghrelin designed to improve glycaemic control and reduce weight.
PPTN is a potent, highly specific amtagonist of P2Y14 receptor with Ki of 0.4 nM in functional assays; exhibits no agonist or antagonist effect at the P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, or P2Y13 receptors at 1 uM; inhibits UDP-glucose-stimulated chemotaxis of human neutrophils.
Urapidil-d4 is the deuterium labeled Urapidil[1]. Urapidil is an α1 adrenoreceptor antagonist and a 5-HT1A receptor agonist[2].
Fexofenadine is a third-generation antihistamine pharmaceutical drug used in the treatment of allergy symptoms, such as hay fever, nasal congestion, and urticaria.
Dehydroaripiprazole-d8 is deuterium labeled Dehydroaripiprazole. Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole. Dehydroaripiprazole has with antipsychotic activity equivalent to Aripiprazole[1][2][3].
Pentoxyverine-d8 (Carbetapentane-d8) is the deuterium labeled Pentoxyverine. Pentoxyverine (Carbetapentane) is a sigma-1 receptor agonist, with a Ki of 75 nM on guinea-pig brain membranes. Pentoxyverine is a centrally-acting cough suppressant with antimuscarinic and anticonvulsant properties. Pentoxyverine can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance[1][2][3][4].
WAY 208466 dihydrochloride is a potent and selective 5-HT6 receptor agonist (EC50=7.3 nM for the human 5-HT6 receptor). WAY-208466 dihydrochloride elevates cortical GABA levels in rat frontal cortex[1]. WAY 208466 dihydrochloride exhibits antidepressant and anxiolytic-like effects[2].
ARS-1620 is an atropisomeric selective KRASG12C inhibitor with desirable pharmacokinetics.
Travoprost is used to treat glaucoma and ocular hypertension.Target: OthersTravoprost ophthalmic solution is a topical medication used for controlling the progression of glaucoma or ocular hypertension, by reducing intraocular pressure. It is a synthetic prostaglandin analog (or more specifically, an analog of prostaglandin F2α) that works by increasing the outflow of aqueous fluid from the eyes. From Wikipedia.
AP5 sodium is a potent, orall active, and selective GPR40 receptor agonist with a positive allosteric modulation of endogenous ligand (AgoPAM). AP5 sodium demonstrates rat and human inositol monophosphate (IP1) EC50 values of 0.49 nM and 0.8 nM against the GPR40 receptor, respectively. AP5 sodium has the potential for type II diabetes research[1].
Allantoin-13C2,15N4 is the 13C and 15N labeled Allantoin[1]. Allantoin is a skin conditioning agent that promotes healthy skin, stimulates new and healthy tissue growth[2].
KRAS G12C inhibitor 35 is a potent inhibitor of KRAS G12C. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12C inhibitor 35 has the potential for the research of KRAS G12C-mediated cancer (extracted from patent CN112920183A, compound 3)[1].
MIPS521 is a positive allosteric modulator of adenosine A1 receptor (A1AR). MIPS521 also has a lower A1R allosteric affinity (pKB=4.95). MIPS521 exhibits pain-relieving effects in vivo[1][2].
KSK68 is a high-affinity dual sigma-1 and histamine H3 receptor antagonist, with Kis of 7.7, 3.6, 22.4 nM for H3 receptor, sigma-1, sigma-2 receptor respectively. KSK68 has negligible affinity at the other histamine receptor subtypes. KSK68 can be used for research of nociceptive and neuropathic pain[1].
Urocortin II, mouse is a potent and selective endogenous peptide agonist of type-2 corticotropin-releasing factor (CRF2) receptor with Ki values of 0.66 nM and ﹥100 nM for CRFR2 and CRFR1, respectively. Urocortin II, mouse activates CRF2 receptors in a cAMP/PKA- and Ca2+/CaMKII-dependent manner.Urocortin II, mouse is expressed in discrete areas of the central nervous system, and activates central neurons involved in the processing of visceral sensory information, and in modulating autonomic outflow[1][2][3].
CXCR4 antagonist 2 is a CXCR4 antagonist with an IC50 value of 47 nM.
Aclerastide (DSC-127) is an angiotensin receptor agonist. Aclerastide also is a peptide analog of angiotensin II. Aclerastide can be used for the research of tissue regeneration in diabetic ulcers[1][2].
Lixisenatide acetate is a glucagon-like peptide-1 (GLP-1) receptor agonist that can be used in the treatment of type 2 diabetes mellitus (T2DM).
Pranlukast-d4 is deuterium labeled Pranlukast. Pranlukast is a highly potent, selective and competitive antagonist of peptide leukotrienes. Pranlukast inhibits [3H]LTE4, [3H]LTD4, and [3H]LTC4 bindings to lung membranes with Kis of 0.63±0.11, 0.99±0.19, and 5640±680 nM, respectively.
CR 665 (JNJ 38488502) is a peripherally selective κ-opioid agonist. CR 665 can activate the kappa opioid receptor with EC50 value of 10.9 nM. CR 665 can be used for the research of peripheral pain[1][2].
Mepyramine maleate, a first generation antihistamine, is an antagonist of histamine H1 receptor, with Kds of 0.8 nM, 5200 nM and >3000 nM for H1, H2, and H3 receptor, respectively, and a pKd of 9.4 for H1 receptor.
KRAS G12C inhibitor 33 is a KRAS G12C inhibitor extracted from patent WO2021244603A1, compound 1. KRAS G12C inhibitor 33 can be used for the research of cancer[1].
(D-Phe6,Leu-NHEt13,des-Met14)-Bombesin (6-14) is a bombesin (BBN) antagonist and can be used for the research of cancer[1].
Latanoprost acid, an analog of prostaglandin (PG) F2α, is an selective prostanoid receptor (FP) agonist that specifically activates the FP-PG receptor[1]. Latanoprost acid inhibits RANKL-induced osteoclastgenesis and function by inhibiting ERK, AKT, JNK, and p38 cascade, following by the c-fos/NFATc1 pathway. Latanoprost acid is a medication which works to lower pressure inside the eyes[2].
MCOPPB 3Hcl is a nociceptin receptor agonist with pKi of 10.07; weaker activity at other opioid receptors.IC50 value: 10.07 (pKi)Target: nociceptin receptorMCOPPB trihydrochloride is a trihydrochloride form of MCOPPB that is a new nonpeptide nociceptin/orphanin FQ peptide (NOP)-receptor agonist with a pKi of 10.07 ± 0.01 for the human NOP receptor.
Neuropeptide S(Rat) is a potent endogenous neuropeptide S receptor (NSPR) agonist (EC50=3.2 nM). Neuropeptide S(Rat) increases locomotor activity and wakefulness in mice. Neuropeptide S(Rat) also reduces anxiety-like behavior in mice.
CB2R/FAAH modulator-1 is a cannabinoid type 2 receptor (CB2R) full agonist with Kis of 14.8 nM and 241.3 nM for CB2R and CB1R, respectively. CB2R/FAAH modulator-1 is a fatty acid amide hydrolase (FAAH) inhibitor with an IC50 of 4 μM. CB2R/FAAH modulator-1 decreases pro-inflammatory and increases anti-inflammatory cytokines production[1].
Naftopidil hydrochloride (KT-611 hydrochloride) is a selective alpha1-adrenoceptor antagonist, with antiproliferative effects. Naftopidil dihydrochloride can be used for the research of prostate hyperplasia[1].
PF-232798 is an orally active CCR5 antagonist with anti-HIV effects[1].