Catalog No.
Product Name
Application
Product Information
Citations
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MC1R and MC5R antagonist
JNJ-10229570 is a novel MC1R and MC5R antagonist was used to treat primary human sebaceous cells. -
α1A antagonist
RS 17053 HCl is α1A-adrenoceptor antagonist, with very high affinity for α1A receptors (pKi and pA2 estimates of 9.1 - 9.9) and a 30 - 100 fold selectivity over the α1B and α1D subtypes (pKi and pA2 estimates 7.7 - 7.8). -
Endogenous galanin receptor agonist
Galanin (1-30) (human) is an endogenous peptide with multiple endocrine, metabolic and behavioral effects - Glucagon-Like Peptide 1 (7-36) Amide is a potent glucose-dependent insulinotropic peptide produced by post-translational processing of proglucagon in intestinal L-cells.
- Ying Zhou, .et al. , Adv Biol (Weinh), 2022, Nov 14 PMID: 36373695
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MOR agonist
SR17018 is an mu-opioid-receptor (MOR) agonist with an EC50 of 97 nM.- Rob Hill, .et al. , Br J Pharmacol, 2023, Jul 24 PMID: 37489013
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NK1 receptor antagonist
Tradipitant, also known as VLY-686 and LY686017, is the 2nd generation neurokinin-1 receptor antagonist, which showed activity in preclinical anxiety models. -
KOR agonist
Asimadoline is a potent κ-opioid receptor (KOR) agonist (IC50s = 5.6 and 1.2 nM for guinea pig and human receptors, respectively). -
CGRP receptor antagonist
HCGRP-(8-37) is a human calcitonin gene-related peptide (hCGRP) fragment and also an antagonist of CGRP receptor.
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CRF-1 antagonist
Verucerfont, also known as GSK561679 and NBI77860, is a CRF-1 antagonist. Verucerfont blocks the CRH-1 receptor, and so reduces ACTH release following chronic stress. -
5-HT6 receptor antagonist
SB 399885 is a potent, brain penetrant, and orally active SR-6 antagonist. It displays > 200-fold selectivity for SR-6 over other serotonin receptors (pKi values are 9.11, 8.81 and 9.02 for human recombinant, native rat and native human SR-6 receptors, respectively).
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DP1 receptor antagonist
Asapiprant, also known as S-555739, is a the potent and selective DP1 receptor antagonist. Asapiprant exhibited high affinity and selectivity for the DP1 receptor. -
GLP-1 receptor agonist
Dulaglutide is a glucagon-like peptide-1 (GLP-1) receptor agonist.- Liuqing Xi, .et al. , Peptides, 2025, Mar:185:171366 PMID: 39954860
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5-HT1F antagonist
LY 334370 hydrochloride is a selective 5-HT1F receptor agonist (Ki values are 1.87, 16.4, > 100 (IC50)). CAS: 199673-74-0(LY 334370 hydrochloride); 182563-08-2 (LY 334370 Free Base) -
H4 receptor antagonist
JNJ-39758979 is histamine H4 receptor antagonists with a Ki of 12.5 nM. -
5-HT(2A) receptor agonist
Temanogrel, also known as APD791, is a highly selective 5-hydroxytryptamine2A receptor inverse agonist under development for the treatment of arterial thrombosis. -
opioid receptor antagonis
Bevenopran, also known as CB-5945, ADL-5945, MK-2402, OpRA III, is a peripherally selective μ- and δ-opioid receptor antagonist. -
5-HT2A receptor antagonist
Volinanserin is a highly selective 5-HT2A receptor antagonist.- Hugo R Arias, .et al. , Eur J Pharmacol, 2024, Mar 5:966:176329 PMID: 38253116
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OX2 receptor antagonist
TCS-OX2-29 is a selective OX2 receptor antagonist with IC50 value of 40 nM. CAS: 1610882-30-8 (HCl) 372523-75-6 (Free Base) -
IP (prostacyclin) receptor antagonist
RO-1138452 is a potent and selective IP (prostacyclin) receptor antagonist with high affinity for IP receptors. -
sigma1 receptor agonist
Anavex2-73 is a muscarinic/moderate sigma1 receptor agonist that alleviated the scopolamine- and dizocilpine-induced learning impairments. CAS: 195615-83-9 (Free base) 195615-84-0 (HCl) -
histamine H3 receptors agonist
S38093 is an inverse agonist at histamine H3 receptors. CAS: 862896-30-8 (Free base) 1222097-72-4 (HCl) -
CRTh2 receptor antagonist
Fevipiprant, also known as NVP-QAW039 or QAW039, is an oral active and potent CRTh2 receptor antagonist and potentially useful for asthma treatment. -
beta-adrenergic receptor antagonist
Nifenalol, also known as INPEA, is a new beta-adrenergic receptor antagonist. -
α-adrenoceptor agonist
Xylometazoline hydrochloride is an α-adrenoceptor agonist commonly used as nasal decongestant. -
alpha-adrenergic receptor agonist / MAO inhibitor
Amitraz, also known as Mitaban and Taktic, is an alpha-adrenergic receptor agonist and MAO inhibitor used as an insecticide in prevention of flea and tick infections. It prevents prostaglandin synthesis and may inhibit beta-cell insulin release. -
5-HT2 antagonist
Sarpogrelate hydrochloride (MCI-9042), a selective 5-HT2 antagonist, has been widely used as an anti-platelet agent for the treatment of PAD. - Harmine, also known as telepathine, is a fluorescent harmala alkaloid belonging to the beta-carboline family of compounds. It occurs in a number of different plants, most notably the Middle Eastern plant harmal or Syrian rue (Peganum harmala) and the South American vine Banisteriopsis caapi (also known as "yage" or "ayahuasca"). Harmine reversibly inhibits monoamine oxidase A (MAO-A), an enzyme which breaks down monoamines, making it a RIMA. Harmine selectively binds to MAO-A but does not inhibit the variant MAO-B.
- Fariha Karim, .et al. , Synapse, 2025, Jul;79(4):e70024 PMID: 40619690
- Lei Tan, .et al. , Res Vet Sci, 2022, 145: 125-134 PMID: 35190327
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D2DR and D4DR inhibitor
Loxapine Succinate is a D2DR and D4DR inhibitor and serotonergic receptor antagonist. Loxapine succinate is an antipsychotic agent used in schizophrenia. -
MT1 and MT2 receptor agonist
Tasimelteon is a melatonin MT1 and MT2 receptor agonist. -
β-adrenergic receptor antagonist
(R)-Atenolol is a beta blocker used to treat high blood pressure and chest pain (angina). It can also reduce the risk of death after a heart attack. -
β2AR agonist
Metaproterenol hemisulfate (Orciprenaline hemisulfate) is a direct-acting sympathomimetic and a β2-adrenergic receptor (β2AR) agonist with an IC50 of 68 nM. Metaproterenol hemisulfate also has anti-inflammatory activity. -
alpha-1 adrenergic agonist
Methoxamine Hydrochloride is an alpha-1 adrenergic agonist that causes prolonged peripheral vasoconstriction. -
Non-selective β antagonist
Oxprenolol is an orally bioavailable β-adrenergic receptor (β-AR) antagonist (Ki = 7.10 nM in a radioligand binding assay using rat heart tissue). It is non-selective and inhibits both β1- and β2-ARs (Kds = 2.09 and 1.35 nM in isolated rat heart and uterus, respectively). Oxprenolol is selective for β-ARs over serotonin (5-HT) receptors in rat sarcolemmal membrane preparations (IC50s = 4.13 and 23,300 nM, respectively), but it binds to 5-HT1A receptors in rat hippocampus and 5-HT1B in rat striatum (Kis = 94.2 and 642 nM, respectively). -
beta-Adrenergic agonist
Ractopamine HCl is a beta-Adrenergic agonist. It acts by being a full agonist at the TAAR1. -
H1 histamine receptor antagonist
Terfenadine ((??)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9 and induces p73, Noxa. - Misoprostol is a medication used to start labor, cause an abortion, prevent and treat stomach ulcers, and treat postpartum bleeding due to poor contraction of the uterus. For abortions it is often used with mifepristone or methotrexate. By itself effectiveness for this purpose is between 66% and 90%.
