Orphan GPCR

Rrphan G protein-coupled receptor

Orphan GPCRs (orphan G protein-coupled receptors) are receptors lacking endogenous ligands. GPCRs are th largest family of transmembrane receptors and have over the past decades developed into highly successful drug targets. However, many GPCRs are still orphans and the function is enigmatic. Orphan GPCRs account for ∼30% of the ∼400 non-olfactory human GPCRs. In terms of orphan GPCR ligands, initial efforts focused on identifying novel neuropeptides since orphan GPCR expression was located primarily in the brain. G protein coupling of unliganded orphan GPCRs—GPR22, GPR137b, GPR88, GPR156, GPR158, GPR179, GPRC5D and GPRC6A—with pathophysiological association were accurately detected using luciferase reporter assays^[1]^[2].

References:

[1]. Wang T, et, al. Orphan GPCR GPRC5C Facilitates Angiotensin II-Induced Smooth Muscle Contraction . Circ Res. 2024 May 10;134(10):1259-1275. [Content Brief]

[2]. Jobe A, et, al. Orphan G protein-coupled receptors: the ongoing search for a home. Front Pharmacol. 2024 Feb 29:15:1349097. [Content Brief]

Orphan GPCR Related Products (23):

By Effects:	Inhibitors (8) Agonists (7) Ligands (2) Antagonists (4)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-160187

AAA	Antagonist	99.52%
AAA is an orally active 20-HETE receptor antagonist. AAA exerts antihypertensive and organoprotective effects. AAA blocks 20-HETE prohypertensive actions, suppresses intrarenal and circulating angiotensin II levels, and interferes with renin-angiotensin system interactions. AAA attenuates development of, and reverses established, ANG II (HY-13948)-dependent malignant hypertension. AAA reduces albuminuria, glomerulosclerosis, and cardiac hypertrophy linked to malignant hypertension. AAA can be used for the research of malignant hypertension.

HY-156815

YL-365	Antagonist	99.96%
YL-365 is a potent and selective GPR34 antagonist with an IC₅₀ of 17 nM. YL-365 binds to a portion of the orthosteric binding pocket of GPR34 and induces allosteric changes that stabilize the receptor in an inactive conformation. YL-365 down-regulates expression of the proinflammatory gene iNOS in M1 microglia and suppresses proinflammatory responses. YL-365 reduces mechanical allodynia in a dose-dependent manner in a mouse model of neuropathic pain. YL-365 can be used for the research of neuropathic pain.

HY-12664

AF64394	Inhibitor	98.02%
AF64394 is a GPR3 inverse agonist, with a pIC₅₀ of 7.3.

HY-N15721

Tryptophan-cholic acid	Agonist	99.75%
Tryptophan-cholic acid (Trp-CA) is a microbial amino acid-conjugated bile acid that acts as an endogenous ligand and agonist (EC₅₀=9.6 μM) for the orphan G protein-coupled receptor (GPCR) MRGPRE (Mas-related G protein-coupled receptor family member E). Tryptophan-cholic acid is orally effective but has poor oral absorption and does not cross the blood-brain barrier. Tryptophan-cholic acid promotes the secretion of glucagon-like peptide GLP-1, thereby improving glucose tolerance in diabetic mice. Tryptophan-cholic acid improves glucose tolerance, promotes insulin secretion, and alleviates high-fat diet-induced hepatic steatosis without causing pruritus side effects. Tryptophan-cholic acid is primarily used in research on type 2 diabetes (T2D).

HY-155318A

GPR3 agonist-2	Agonist	99.90%
GPR3 agonist-2(compound 32) is a potent full agonist of G protein-coupled receptor 3, with the IC₅₀of 260 nM.

HY-P991805

Anti-Mouse F4/80 Antibody (Cl:A3-1)	Inhibitor
Anti-Mouse F4/80 Antibody (Cl:A3-1) reacts with the mouse F4/80. The F4/80 receptor is generally considered a murine pan-macrophage marker. Recommend Isotype Controls: Rat IgG2b kappa, Isotype Control (HY-P990682).

HY-107752A

GPR17 agonist 1	Agonist
GPR17 agonist 1 is a selective and potent GPR17 agonist with an EC₅₀ of 35 pM. GPR17 agonist 1 also shows weak activation of P2Y Receptor. GPR17 agonist 1 can be used for the research of neurological disease.

HY-P991934

Anti-CD97 Antibody
Anti-CD97 Antibody is an antibody against human CD97.

HY-155417

GPR34 receptor antagonist 3	Antagonist	99.88%
GPR34 receptor antagonist 3 (Compound 5e) is a class of GRP34 antagonists, IC₅₀ is 0.680 μM. GPR34 receptor antagonist 3 inhibited ERK1/2 phosphorylation induced by lysophosphatidylserine in a dose-dependent way without obvious cytotoxicity. GPR34 receptor antagonist 3 shows antisensory activity in mouse neuropathic pain model .

HY-156354

GPR61 Inverse agonist 1	Inhibitor	98.24%
GPR61 Inverse agonist 1 (Compound 1) is a GPR61 inverse agonist (IC₅₀: 11 nM). GPR61 Inverse agonist 1 can be used for research of disorders of metabolism and body weight, such as obesity and cachexia.

HY-163087

PT-91	Agonist	98.78%
PT-91 is an agonist of GPR27. PT-91 exhibits high metabolic stability and brain exposure in mice.

HY-114146

CID 1375606	Agonist	99.90%
CID 1375606 is a surrogate agonist of orphan G protein-coupled receptor GPR27.

HY-110114

Gue1654	Inhibitor	98.31%
Gue1654 is a modulator of OXE-R. Gue1654 inhibits Gβγ but not Gα signaling triggered upon activation of Gα(i)-βγ by the chemoattractant receptor OXE-R. Gue1654 does not interfere nonspecifically with signaling directly at or downstream of Gβγ.

HY-P991726

Vemzatatug	Inhibitor
Vemzatatug is a humanized IgG1κ monoclonal antibody inhibitor targeting GPRC5D. Vemzatatug has an antitumor activity. Vemzatatug can be used for cancers like multiple myeloma (MM) research.

HY-W693142

Succinate calcium	Ligand
Succinate calcium is a key intermediate product of the citric acid cycle (tricarboxylic acid cycle). Succinate calcium can act as a specific ligand for the G protein-coupled receptor GPR91. Succinate calcium can increase the amplitude of calcium transient in cardiac muscle cells and accelerate the decay rate of calcium transient. Succinate calcium can induce myocardial apoptosis.

HY-182271

GPR61 Inverse agonist 3	Inhibitor
GPR61 Inverse agonist 3 is a selective and brain-penetrant GPR61 inverse agonist with human IC₅₀ of 4.0 nM, mouse IC₅₀ of 8.8 nM, human K_i of 0.34 nM, mouse K_i of 1.1 nM. GPR61 Inverse agonist 3 disrupts GPR61-Gαs protein interactions to abolish GPR61 constitutive activity. GPR61 Inverse agonist 3 moderately inhibits GABA_A chloride channel and PDE3A1 with IC₅₀ values of 4.6 and 8.9 μM. GPR61 Inverse agonist 3 shows no functional effect on food intake in adult mice co-administered with a pan-CYP inhibitor. GPR61 Inverse agonist 3 can be used for the research of cachexia/sarcopenia.

HY-P5762A

Phoenixin-14 TFA	Ligand
Phoenixin-14 (PNX-14) TFA is an endogenous neuropeptide with multiple biological activities, and serves as the endogenous ligand of GPR173. Phoenixin-14 TFA reduces ROS production by inhibiting the HMGB1/TLR4/MyD88/NF-κB signaling axis, thereby exerting antioxidant and mitochondrial protective effects. Phoenixin-14 TFA inhibits FOXO3 phosphorylation by upregulating SIRT3 expression, suppresses apoptosis, and improves myocardial systolic/diastolic function. Phoenixin-14 TFA resists ferroptosis by activating the ATF4/SLC7A11/GPX4 axis; it activates ERK1/2 phosphorylation via GPR173. Phoenixin-14 TFA can be used in researches on neuroprotection, diabetes, cardiomyopathy, reproductive protection and so on.

HY-125313

PSB-1737	Agonist
PSB-1737 is a human-selective GPR17 agonist with an EC₅₀ for human GPR17 of 270 nM, and its activity on murine GPR17 is relatively weak (EC₅₀ > 10 μM). PSB-1737 shows no significant inhibition at the glycine binding site of NMDA receptors, and has no significant agonistic or antagonistic activity on P2Y receptor subtypes. PSB-1737 can be used in demyelinating diseases (such as multiple sclerosis) or inflammatory-related anemia.

HY-P992226

Anti-EMR2 Antibody
Anti-EMR2 Antibody is a monoclonal antibody targeting ADGRE2. It can be used in ELISA, FACS, and functional assays. For isotype controls of Anti-EMR2 Antibody, please refer to Human IgG1 kappa, Isotype Control (HY-P99001).

HY-164641

GPR34 agonist 1	Agonist
GPR34 agonist 1 (Compound M1), a lysophosphatidylserine analogue, is an efficient GPR34 agonist.

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