Syk Inhibitor II dihydrochloride is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II dihydrochloride inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II dihydrochloride shows less potent against other kinases and has anti-allergic effect[1].
TUS-007 is a CANDDY molecular, modified from a proteasome inhibitor. However, TUS-007 hardly inhibits proteasome activity. TUS-007 is also an orally active and potent KRAS G12D/V degrader. TUS-007 can be applied in KRAS G12D/V chemical knockdown in cell-free. TUS-007 also exhibits tumor suppression[1]. Note: CANDDY refers to Chemical knockdown with Affinity aNd Degradation DYnamics.
Chloropyramine is competitive reversible H1 receptor antagonist. Chloropyramine also has anti-tumour activity in breast cancer. Chloropyramine can be used for the research of allergic conditions, such as conjunctivitis and bronchial asthma[1][2].
4-Hydroxypropranolol D7 hydrochloride ((±)-4-hydroxy Propranolol D7 hydrochloride) is a deuterium labeled 4-Hydroxypropranolol hydrochloride. 4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol, with potency comparable to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA2 values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties[1][2][3].
Emoghrelin, isolated from? Heshouwu Polygonum multiflorum, stimulates growth hormone secretion via activation of the ghrelin receptor[1].
Metoprolol-d5 is the deuterium labeled Metoprolol[1]. Metoprolol is an orally active, selective β1-adrenoceptor antagonist. Metoprolol shows anti-inflammation, antitumor and anti-angiogenic properties[2][3][4].
Benzamide Derivative 1 is a benzamide derivative from patent EP0213775A1, compound 18. Benzamide Derivative 1 may be useful in treatment of gastrointestinal disorders.
Pregnenolone monosulfate acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, reduces several effects of tetrahydrocannabinol (THC).
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).
Denopamine ((R)-(-)-Denopamine) is an orally active, selective β1-adrenergic agonist. Denopamine prolongs survival in a murine model of congestive heart failure induced by viral myocarditis: suppression of tumor necrosis factor-α production in the heart. Cardiovascular effects[1].
LY306669 is a potent and selective leukotriene B4 (LTB4) receptor antagonist that can be used for the research of lung injury[1].
Aclidinium Bromide(LAS 34273; LAS-W 330) is a long-acting, inhaled muscarinic antagonist as a maintenance treatment for chronic obstructive pulmonary disease (COPD). IC50 value:Target: M3 receptorPreclinically, aclidinium showed potent antagonism of human muscarinic receptors, with a long residence time at M3 receptors and a shorter residence time at M2 receptors, indicating the potential to provide sustained bronchodilation. Aclidinium is rapidly hydrolysed in human plasma, unlike other currently available antimuscarinics including tiotropium. Early clinical studies in healthy subjects have confirmed the low systemic bioavailability and favourable safety profile of single and multiple doses of aclidinium. In a subsequent Phase IIb study, which included 464 patients with moderate to severe COPD, aclidinium displayed long-lasting bronchodilatory activity and was well tolerated.
Apraclonidine hydrochloride (ALO 2145), a selective α2 and weak α1 receptor agonist activity, effectively lowers intraocular pressure (IOP) in human eyes. Apraclonidine hydrochloride is a topical ophthalmic solution[1][2].
[Ala17]-MCH, a MCH analogue (HY-P1525A), is a selective ligand for MCHR1 (Ki=0.16 nM) over MCHR2 (Ki=34 nM). [Eu3+ chelate-labeled [Ala17]-MCH shows high affnity for MCHR1 (Kd=0.37 nM) while has little demonstrable binding affnity for MCHR2[1].
Methylergometrine (Methylergonovine) is an orally active 5-HT2B ligand agonist. Methylergometrine can be used as oxytocin and has protective effect on postpartum hemorrhage[1][2][3].
RBC8 is a novel small molecule inhibitor of Ral GTPase; has IC50 of 3.5 μM in H2122 cell and 3.4 μM in H358 cell.IC50 value:Target: Ral GTPase inhibitorRBC8 or BQU57 treatment showed no further inhibition of colony formation after Ral knockdown. RBC8 and BQU57 showed favorable properties that define good drug candidates. To test the effect of Ral inhibitors on xenograft tumor growth, nude mice were inoculated subcutaneously with H2122 human lung cancer cells and treated intraperitoneally with 50 mg/kg/d of RBC8 for 21 days (except weekends). RBC8 inhibited tumor growth to a similar extent as dual knockdown of RalA and RalB.
Deoxycholic acid sodium salt is specifically responsible for activating the G protein-coupled bile acid receptor TGR5 that stimulates brown adipose tissue (BAT) thermogenic activity.
LY3027788 hydrochloride, a diester analog of LY3020371 which is an mGlu2/3 receptor antagonist, is a potent and orally active prodrug of LY3020371. LY3027788 hydrochloride has antidepressant efficacy[1][2].
Alniditan (Alnitidan) dihydrochloride is a potent 5-HT1B and 5-HT1D receptors agonist, with IC50s of 1.7 nM and 1.3 nM for h5-HT1B and h5-HT1D receptors in HEK 293 cells, respectively. Alniditan dihydrochloride has migraine-preventive effects[1][2].
(-)-Camphoric acid is the less active enantiomer of Camphoric acid. Camphoric acid stimulates osteoblast differentiation and induces glutamate receptor expression. Camphoric acid also significantly induced the activation of NF-κB and AP-1[1].
(+)-N-Allylnormetazocine ((+)-SKF 10047) hydrochloride is a benzomorphan opioid with psychotomi metic effects. (+)-N-Allylnormetazocine hydrochloride is an opioid receptor antagonist with Ki values of 300 nM and 27 μM for σ1 and σ2 opioid receptors, respectively. (+)-N-Allylnormetazocine hydrochloride can be used for the research of neurological disease[1][2].
KSK67 is a high-affinity dual sigma-2 and histamine H3 receptor antagonist, with Kis of 3.2, 1531, 101 nM for H3 receptor, sigma-1, sigma-2 receptor respectively. KSK67 can be used for research of nociceptive and neuropathic pain[1].
Dimethindene is a potent, selective histamine H1 antagonist. Dimethindene impairs cutaneous wound healing (WH). Dimethindene can block K+ currents[1][2].
Xamoterol hemifumarate is a selective and potent agonist of beta1-adrenergic receptor. Xamoterol hemifumarate has the potential for the research of arrhythmogenesis. Xamoterol hemifumarate has the potential for the investigating the relationship between β1-adrenergic stimulation and IKr[1].
Zolertine hydrochloride is an α-adrenoceptor antagonist with a pKi of 6.81 in rat liver (α1B-adrenoceptors) and 6.35 in rabbit liver (α1A-adrenoceptors) membranes[1].
GR 89696 free base is a highly selective κ2 opioid receptor agonist with potential to prevent pruritus[1].
HAEGTFTSDVS is the first N-terminal 1-11 residues of GLP-1 peptide.
BIMU 8 is a potent and selective 5-HT4 agonist with EC50s of 18 nM, 77 nM, and 540 nM for wild type 5HT4 receptor, T3.36A, and W6.48A mutant 5-HT4 receptors[1][2].