GPR
阻害剤の選択性比較
| カタログ番号 | 製品カタログ | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | アルコール | ||
| S7263 | AZD1981 | <1 mg/mL | 11 mg/mL | <1 mg/mL |
| S0851 | G-1 | <1 mg/mL | 82 mg/mL | '''<1 mg/mL |
| S6850 | NE 52-QQ57 | <1 mg/mL | 12 mg/mL | 50 mg/mL |
| S0135 | JMS-17-2 | <1 mg/mL | 40 mg/mL | 10 mg/mL |
| S6651 | G15 (GRB-G15) | <1 mg/mL | 74 mg/mL | ''<1 mg/mL |
| S2822 | OC000459 | <1 mg/mL | 4 mg/mL | <1 mg/mL |
| S2637 | Fasiglifam (TAK-875) | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S2149 | GSK1292263 | <1 mg/mL | 34 mg/mL | <1 mg/mL |
| S8014 | GW9508 | <1 mg/mL | 69 mg/mL | 69 mg/mL |
| S0001 | GSK137647A | <1 mg/mL | 61 mg/mL | '10 mg/mL |
| S6889 | Monomethyl Fumarate | 20 mg/mL | 26 mg/mL | 26 mg/mL |
| S0208 | 6-OAU | <1 mg/mL | 35 mg/mL | <1 mg/mL |
| S0156 | CID 1375606 | <1 mg/mL | 77 mg/mL | <1 mg/mL |
| S0110 | APD597 | <1 mg/mL | 96 mg/mL | <1 mg/mL |
| S6759 | TC-G-1008 (GPR39-C3) | <1 mg/mL | 84 mg/mL | 2 mg/mL |
| S6746 | APD668 | <1 mg/mL | 96 mg/mL | 2 mg/mL |
| S5400 | 3-chloro-5-hydroxybenzoic Acid | -1 mg/mL | 34 mg/mL | -1 mg/mL |
| S8673 | ONC212 | <1 mg/mL | 88 mg/mL | 88 mg/mL |
| S6425 | JNJ 63533054 | -1 mg/mL | 63 mg/mL | -1 mg/mL |
GPR製品
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S7263 |
AZD1981AZD1981 is a potent, selective CRTh2 (DP2) receptor antagonist with IC50 of 4 nM, showing >1000-fold selectivity over more than 340 other enzymes and receptors, including DP1. Phase 2. |
||
| S0851新 |
G-1G-1 is a nonsteroidal and selective agonist of G protein-coupled receptor 30 (GPR30, G protein-coupled estrogen receptor 1, GPER) with Ki of 11 nM. |
||
| S6850新 |
NE 52-QQ57NE 52-QQ57 is a selective, and orally available antagonist of G-protein coupled receptor 4 (GPR4) with IC50 of 0.07 μM. NE 52-QQ57 effectively blocks GPR4-mediated cAMP accumulation with IC50 of 26.8 nM in HEK293 cells. The antagonism of GPR4 with NE 52-QQ57 significantly inhibits the AGE-induced increased expression of several key inflammatory cytokines and signaling molecules, including tumor necrosis factor-α (TNF-α), interleukin (IL)-1β, IL-6, inducible nitric oxide synthase (iNOS), nitric oxide (NO), cyclooxygenase 2 (COX2), and prostaglandin E2 (PGE2). |
||
| S0135新 |
JMS-17-2JMS-17-2 is a potent and selective small-molecule antagonist of CX3C chemokine receptor 1 (CX3CR1/GPR13) with IC50 of 0.32 nM. JMS-17-2 is used in the research of metastatic disease in breast cancer patients. |
||
| S6651 |
G15 (GRB-G15)G15 is a cell-permeable high affinity and selective G-protein coupled estrogen receptor 1 (GPER, GPR30) antagonist with an affinity of approximately 20 nM that displays no affinity for ERα and ERβ at concentrations up to 10 μM. |
||
| S2822 |
OC000459OC000459 is a potent and selective D prostanoid receptor 2 (DP2) antagonist with IC50 of 13 nM. Phase 2. |
||
| S2637 |
Fasiglifam (TAK-875)Fasiglifam (TAK-875) is a selective GPR40 agonist with EC50 of 14 nM in human GPR40 expressing CHO cell line, 400-fold more potent than oleic acid. |
INS-1 cells were incubated with 50 uM palmitate or BSA in the presence or absence of 5 uM TAK 875 for 30 min, followed by stimulation with 16.6 mm [U-13C]glucose for 30 min. Under these conditions, the following were measured: fructose bisphosphate (FBP) (I), NADH/NAD+ ratio (J). Error bars represent mean ?S.E. n = 3-4.
|
|
| S2149 |
GSK1292263GSK1292263 is a novel GPR119 agonist, showing potential for the treatment of type 2 diabetes. Phase 2. |
(B) WB403 at 10, 20 μmol/l had no significant stimulation effect on hGPR119 dependent cAMP accumulation. GSK1292263 (1 μmol/l) was used as positive agonist of GPR119.
|
|
| S8014 |
GW9508GW9508 is a potent and selective agonist for FFA1 (GPR40) with pEC50 of 7.32, 100-fold selective against GPR120, stimulates insulin secretion in a glucose-sensitive manner. |
||
| S0001新 |
GSK137647AGSK137647A (GSK 137647) is a selective, non-carboxylic agonist of free fatty acid receptor 4 (FFA4/GPR120) with EC50 of 501 nM. |
||
| S6889新 |
Monomethyl FumarateMonomethyl Fumarate (MMF, Monomethylfumarate, Fumaric acid monomethyl ester, Methyl hydrogen fumarate), the active metabolite of the psoriasis drug Fumaderm, is a potent GPR109A agonist. Monomethyl Fumarate prevents major dysfunctions associated with neurodegenerative diseases: oxidative stress, mitochondrial dysfunction, apoptosis and autophagy. |
||
| S0208新 |
6-OAU6-OAU (GTPL5846, 6-n-octylaminouracil) is a surrogate agonist of G protein-coupled receptor 84 (GPR84) that activates human GPR84 in the presence of Gqi5 chimera in HEK293 cells with EC50 of 105 nM in the PI assay. 6-OAU (GTPL5846, 6-n-octylaminouracil) increases [35S]GTPγS incorporated in Sf9 cell membranes expressing human GPR84-Gαi fusion protein with EC50 of 512 nM. |
||
| S0156新 |
CID 1375606CID 1375606 (2,4-Dichloro-N-(phenylcarbamoyl)phenylbenzamide) is an orphan G protein-coupled receptor GPR27 agonist. |
||
| S0110新 |
APD597APD-597 (JNJ-38431055) is a potent and selective G protein-coupled receptor 119 (GPR119) agonist with EC50 of 46 nM for hGPR119 and an inhibitor of Cytochrome P450 2C9 (CYP2C9) with IC50 of 5.8 μM. APD-597 (JNJ-38431055) is developed for treating Type 2 diabetes (T2D). |
||
| S6759新 |
TC-G-1008 (GPR39-C3)TC-G-1008 (GPR39-C3) is a potent and orally available G-protein coupled receptor 39 (GPR39)(zinc receptor) agonist with EC50 of 0.4 nM and 0.8 nM for rat and human receptors, respectively. |
||
| S6746 |
APD668APD668 is a potent GPR119 agonist with EC50s of 2.7 and 33 nM for human and rat forms, respectively. |
||
| S5400 |
3-chloro-5-hydroxybenzoic Acid3-chloro-5-hydroxybenzoic Acid is a selective agonist of the lactate receptor GPR81. |
||
| S8673 |
ONC212ONC212, a fluorinated-ONC201 analogue, is a selective agonist of GPR132. ONC212 is broadly efficacious across most solid tumors and hematological malignancies in the low nanomolar range and has robust anti-leukemic activity. |
||
| S6425 |
JNJ 63533054JNJ 63533054 is a potent and selective GPR139 agonist. It specifically activated human GPR139 in the calcium mobilization (EC50 = 16 ± 6 nM) and GTPγS binding (EC50 = 17 ± 4 nM) assays. |
||
| S4709 |
LatanoprostLatanoprost (Xalatan, PhXA41) is a prostaglandin F2alpha analogue and a prostanoid selective FP receptor agonist with an ocular hypertensive effect. Latanoprost increases uveoscleral outflow and thereby reduces intraocular pressure. |
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S7263 |
AZD1981AZD1981 is a potent, selective CRTh2 (DP2) receptor antagonist with IC50 of 4 nM, showing >1000-fold selectivity over more than 340 other enzymes and receptors, including DP1. Phase 2. |
2019, 18(11):2097-2110 |
|
| S0851新 |
G-1G-1 is a nonsteroidal and selective agonist of G protein-coupled receptor 30 (GPR30, G protein-coupled estrogen receptor 1, GPER) with Ki of 11 nM. |
||
| S6850新 |
NE 52-QQ57NE 52-QQ57 is a selective, and orally available antagonist of G-protein coupled receptor 4 (GPR4) with IC50 of 0.07 μM. NE 52-QQ57 effectively blocks GPR4-mediated cAMP accumulation with IC50 of 26.8 nM in HEK293 cells. The antagonism of GPR4 with NE 52-QQ57 significantly inhibits the AGE-induced increased expression of several key inflammatory cytokines and signaling molecules, including tumor necrosis factor-α (TNF-α), interleukin (IL)-1β, IL-6, inducible nitric oxide synthase (iNOS), nitric oxide (NO), cyclooxygenase 2 (COX2), and prostaglandin E2 (PGE2). |
||
| S0135新 |
JMS-17-2JMS-17-2 is a potent and selective small-molecule antagonist of CX3C chemokine receptor 1 (CX3CR1/GPR13) with IC50 of 0.32 nM. JMS-17-2 is used in the research of metastatic disease in breast cancer patients. |
||
| S6651 |
G15 (GRB-G15)G15 is a cell-permeable high affinity and selective G-protein coupled estrogen receptor 1 (GPER, GPR30) antagonist with an affinity of approximately 20 nM that displays no affinity for ERα and ERβ at concentrations up to 10 μM. |
2020, 38(1):38-46 |
|
| S2822 |
OC000459OC000459 is a potent and selective D prostanoid receptor 2 (DP2) antagonist with IC50 of 13 nM. Phase 2. |
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S2637 |
Fasiglifam (TAK-875)Fasiglifam (TAK-875) is a selective GPR40 agonist with EC50 of 14 nM in human GPR40 expressing CHO cell line, 400-fold more potent than oleic acid. |
2020, 54(6):3428-3436 2019, 2019:5487962 2018, 159(8):2939-2952 |
INS-1 cells were incubated with 50 uM palmitate or BSA in the presence or absence of 5 uM TAK 875 for 30 min, followed by stimulation with 16.6 mm [U-13C]glucose for 30 min. Under these conditions, the following were measured: fructose bisphosphate (FBP) (I), NADH/NAD+ ratio (J). Error bars represent mean ?S.E. n = 3-4.
|
| S2149 |
GSK1292263GSK1292263 is a novel GPR119 agonist, showing potential for the treatment of type 2 diabetes. Phase 2. |
2015, 10(7):e0134051 |
(B) WB403 at 10, 20 μmol/l had no significant stimulation effect on hGPR119 dependent cAMP accumulation. GSK1292263 (1 μmol/l) was used as positive agonist of GPR119.
|
| S8014 |
GW9508GW9508 is a potent and selective agonist for FFA1 (GPR40) with pEC50 of 7.32, 100-fold selective against GPR120, stimulates insulin secretion in a glucose-sensitive manner. |
2020, 99:103830 2020, e2000275 2019, 170:176-186 |
|
| S0001新 |
GSK137647AGSK137647A (GSK 137647) is a selective, non-carboxylic agonist of free fatty acid receptor 4 (FFA4/GPR120) with EC50 of 501 nM. |
||
| S6889新 |
Monomethyl FumarateMonomethyl Fumarate (MMF, Monomethylfumarate, Fumaric acid monomethyl ester, Methyl hydrogen fumarate), the active metabolite of the psoriasis drug Fumaderm, is a potent GPR109A agonist. Monomethyl Fumarate prevents major dysfunctions associated with neurodegenerative diseases: oxidative stress, mitochondrial dysfunction, apoptosis and autophagy. |
||
| S0208新 |
6-OAU6-OAU (GTPL5846, 6-n-octylaminouracil) is a surrogate agonist of G protein-coupled receptor 84 (GPR84) that activates human GPR84 in the presence of Gqi5 chimera in HEK293 cells with EC50 of 105 nM in the PI assay. 6-OAU (GTPL5846, 6-n-octylaminouracil) increases [35S]GTPγS incorporated in Sf9 cell membranes expressing human GPR84-Gαi fusion protein with EC50 of 512 nM. |
||
| S0156新 |
CID 1375606CID 1375606 (2,4-Dichloro-N-(phenylcarbamoyl)phenylbenzamide) is an orphan G protein-coupled receptor GPR27 agonist. |
||
| S0110新 |
APD597APD-597 (JNJ-38431055) is a potent and selective G protein-coupled receptor 119 (GPR119) agonist with EC50 of 46 nM for hGPR119 and an inhibitor of Cytochrome P450 2C9 (CYP2C9) with IC50 of 5.8 μM. APD-597 (JNJ-38431055) is developed for treating Type 2 diabetes (T2D). |
||
| S6759新 |
TC-G-1008 (GPR39-C3)TC-G-1008 (GPR39-C3) is a potent and orally available G-protein coupled receptor 39 (GPR39)(zinc receptor) agonist with EC50 of 0.4 nM and 0.8 nM for rat and human receptors, respectively. |
||
| S6746 |
APD668APD668 is a potent GPR119 agonist with EC50s of 2.7 and 33 nM for human and rat forms, respectively. |
||
| S5400 |
3-chloro-5-hydroxybenzoic Acid3-chloro-5-hydroxybenzoic Acid is a selective agonist of the lactate receptor GPR81. |
||
| S8673 |
ONC212ONC212, a fluorinated-ONC201 analogue, is a selective agonist of GPR132. ONC212 is broadly efficacious across most solid tumors and hematological malignancies in the low nanomolar range and has robust anti-leukemic activity. |
2020, 10(10)E1395 |
|
| S6425 |
JNJ 63533054JNJ 63533054 is a potent and selective GPR139 agonist. It specifically activated human GPR139 in the calcium mobilization (EC50 = 16 ± 6 nM) and GTPγS binding (EC50 = 17 ± 4 nM) assays. |
||
| S4709 |
LatanoprostLatanoprost (Xalatan, PhXA41) is a prostaglandin F2alpha analogue and a prostanoid selective FP receptor agonist with an ocular hypertensive effect. Latanoprost increases uveoscleral outflow and thereby reduces intraocular pressure. |
