| DC46162 |
Vazegepant hydrochloride
Featured
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Vazegepant (BHV-3500) hydrochloride is a highly soluble CGRP receptor antagonist. Vazegepant hydrochloride is the first intranasal gepant for migraine. Vazegepant hydrochloride may be helpful in effective management of COVID-19 associated pulmonary inflammation. |
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| DC46189 |
Teduglutide
Featured
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Teduglutide (ALX-0600, Gattex, Revestive, TAK 633) is an analogue of human glucagon-like peptide-2 (GLP-2) and binds to the GLP-2 receptors. Teduglutide prolongs the intestinotrophic properties of GLP-2 in animal models. |
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| DC46198 |
RVD-Hpα TFA |
RVD-Hpα TFA is the N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. RVD-Hpα TFA increases intracellular Ca2+ levels in cells expressing CB1 receptors in vitro. RVD-Hpα TFA also high affinity CB2 positive allosteric modulator (Ki=50 nM). |
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| DC46208 |
Urocortin II, human |
Urocortin II (human) is a selective endogenous peptide agonist of type-2 corticotropin-releasing factor (CRF2) receptor. For investigating the role of the CRF (2) receptor in ingestive behavior. |
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| DC46209 |
Urocortin II, human TFA |
Urocortin II, human (TFA) is a selective endogenous peptide agonist of type-2 corticotropin-releasing factor (CRF2) receptor. For investigating the role of the CRF (2) receptor in ingestive behavior. |
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| DC46232 |
[Orn5]-URP TFA |
[Orn5]-URP TFA is a potent and selective pure antagonist of Urotensin-II receptor (UT), with an pEC50 of 7.24. [Orn5]-URP TFA displays no agonist activity. |
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| DC46233 |
UFP-803 TFA |
UFP-803 TFA is a potent urotensin-II receptor (UT) ligand. UFP-803 TFA has lower residual agonist activity, so it may be an important tool for the investigations on the role played by the UT system in physiology and pathology. |
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| DC46240 |
CCR4 antagonist 2 |
CCR4 antagonist 2 (Compound 31) is a novel potent, orally bioavailable small molecule antagonists of CC chemokine receptor 4 (CCR4) that inhibits Treg trafficking into the Tumor Microenvironment without suppressing the number of Treg in healthy tissues.
CCR4 antagonist 2 (Compound 31) exhibits IC50 values of Ca2+flux and (chemotaxis) CTX are 40 nM and 70 nM, respectively. |
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| DC46241 |
GPR40/FFAR1 modulator 1(WUN55267)
Featured
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GPR40/FFAR1 modulator 1 is an agonist and an allosteric modulator for Gq-coupled free fatty acid receptor 1 (GPR40/FFAR1). |
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| DC46263 |
Cariprazine D6 |
Cariprazine D6 (RGH-188 D6) is a deuterium labeled Cariprazine. Cariprazine Cariprazine is an antipsychotic agent that exhibits high affinity for the D3 (Ki of 0.085 nM) and D2 (Ki of 0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki of 2.6 nM). |
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| DC46264 |
MGS0274 |
MGS0274, an ester-based lipophilic prodrug of a metabotropic glutamate (mGlu)2 and mGlu3 receptor agonist MGS0008, shows improved oral bioavailability. MGS0274 has the potential for the research of schizophrenia. |
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| DC46287 |
HexylHIBO |
HexylHIBO is a potent group I mGluR antagonist with Kbs of 140 and 110 μM at mGlu1a and mGlu5a receptors, respectively. HexylHIBO decreased sEPSC in rat. |
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| DC46288 |
Dronedarone D6 hydrochloride |
Dronedarone D6 hydrochloride is the deuterium labeled Dronedarone. Dronedarone hydrochloride, a derivative of Amiodarone, is a class III antiarrhythmic agent for the study of atrial fibrillation (AF) and atrial flutter. Dronedarone hydrochloride is a potent blocker of multiple ion currents, including potassium current, sodium current, and L-type calcium current, and exhibits antiadrenergic effects by noncompetitive binding to β-adrenergic receptors. Dronedarone hydrochloride is a substrate for and a moderate inhibitor of CYP3A4.
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| DC46289 |
HEAT hydrochloride |
HEAT (BE2254) hydrochloride is a selective alpha 1 adrenergic receptor antagonist. HEAT hydrochloride, a phenethylamine derivative, shows pKis of 9, 9.1, and 8.57 for alpha 1a, alpha 1b and alpha 1c, respectively. |
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| DC46290 |
Muscarine iodide |
Muscarine ((+)-Muscarine) iodide is a toxin that can stimulate the parasympathetic nervous system. Muscarine iodide is a prototype muscarinic acetylcholine receptor agonist. |
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| DC46291 |
Org37684 |
Org37684 is a highly potent 5-HT2C receptor agonist (pEC50=8.17). Org37684 exhibits a rank order of potency of 5-HT2C>5-HT2B>5-HT2A. Its selectivity for the 5-HT2C receptor is approximately 2.5 times over the 5-HT2B (pEC50=7.96) and ten times for the 5-HT2A (pEC50=7.11) receptor. |
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| DC46339 |
CCZ01048 TFA |
CCZ01048 TFA, a α-MSH analogue, exhibits high binding affinity to melanocortin 1 receptor (MC1R) with a Ki of 0.31 nM. CCZ01048 TFA shows rapid internalization into B16F10 melanoma cells and high in vivo stability. CCZ01048 TFA is a promising candidate for PET imaging of malignant melanoma. |
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| DC46340 |
CCZ01048 |
CCZ01048, a α-melanocyte-stimulating hormone (α-MSH) analogue, exhibits high binding affinity to melanocortin 1 receptor (MC1R) with a Ki of 0.31 nM. CCZ01048 shows rapid internalization into B16F10 melanoma cells and high in vivo stability. CCZ01048 is a promising candidate for PET imaging of malignant melanoma. |
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| DC46345 |
(E/Z)-SIB-1893 |
(E/Z)-SIB-1893 is a racemic compound of (E)-SIB-1893 and (Z)-SIB-1893 isomers. (E)-SIB-1893 is a selective non-competitive metabotropic glutamate subtype 5 receptor (mGluR5) antagonist. |
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| DC46346 |
2-Methoxyidazoxan monohydrochloride |
2-Methoxyidazoxan monohydrochloride (RX821002 hydrochloride) is a highly selective alpha 2-adrenoceptor antagonist with little or no imidazoline antagonist effect. RX 821002 has markedly higher affinity for (guinea-pig) alpha 2D-adrenoceptors (pKd 9.7) than for (rabbit) alpha 2A-adrenoceptors (pKd 8.2). |
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| DC46362 |
Pasireotide acetate |
Pasireotide (SOM230) acetate, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide acetate exhibits antisecretory, antiproliferative, and proapoptotic activity. |
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| DC46376 |
1-Methyl-2-[(6Z,9Z)-6,9-pentadecadienyl]-4(1H)-quinolone |
Methyl-2-[(6Z,9Z)-6,9-pentadecadienyl]-4(1H)-quinolone9 is an antagonist of angiotensin II receptor (IC50=48.2 μM). Methyl-2-[(6Z,9Z)-6,9-pentadecadienyl]-4(1H)-quinolone9 is a quinolone alkaloid from Evodia rutaecarpa. |
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| DC46386 |
Urocortin, rat TFA |
Urocortin, rat TFA (Urocortin (Rattus norvegicus) TFA) is a neuropeptide and a potent endogenous CRFR agonist with Kis of 13 nM, 1.5 nM, and 0.97 nM for human CRF1, rat CRF2α and mouse CRF2β, respectively. |
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| DC46390 |
LY288513 |
LY288513, a selective non-peptide CCK-B receptor antagonist with an IC50 value of 16 nM. LY288513 possesses both anxiolytic and antipsychotic potential. |
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| DC46391 |
PSB-10 hydrochloride |
PSB-10 hydrochloride is a potent and selective antagonist of human adenosine A3 receptor (A3AR), with a Ki of 0.44 nM. PSB-10 hydrochloride shows more than 800-fold selectivity for hA3 over rA1, rA2A, hA1, hA2A and hA2B receptors (Ki=805, 6040, 1700, 2700, 30000 nM, respectively). PSB-10 hydrochloride produces thermal hyperalgesia in mice. |
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| DC46421 |
Gadolinium chloride |
Gadolinium chloride is a specific calcium-sensing receptor (CaSR) agonist. Gadolinium chloride can be used for the research of cardiovascular disease. |
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| DC46423 |
W-84 dibromide |
W-84 (dibromide) is a potent allosteric modulator of M2-cholinoceptors, which retards [3H]N-methylscopolamine dissociation. W-84 dibromide can stabilize cholinergic antagonist-receptor complexes. W-84 (dibromide) is a non-competitive muscarinic acetylcholine receptors antagonist with allosteric effects. W-84 (dibromide) protects over additively against an organophosphate-intoxication when applied in combination with atropine. |
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| DC46433 |
JNJ-39758979 dihydrochloride |
JNJ-39758979 dihydrochloride is a selective, orally active, and high-affinity histamine H4 receptor antagonist, with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 dihydrochloride functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 dihydrochloride shows good anti-inflammatory and antipruritic activity. |
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| DC46444 |
Bupranolol |
Bupranolol is an orally active, competitive and non-selective β-adrenoceptor antagonist without intrinsic sympathomimetic activity. |
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| DC46450 |
CTCE-9908 TFA |
CTCE-9908 TFA is a potent and selective CXCR4 antagonist. CTCE-9908 TFA induces mitotic catastrophe, cytotoxicity and inhibits migration in CXCR4-expressing ovarian cancer cells. |
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