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Áúº´µî¿¡ °ü·ÃµÈ classº° 450¿©°¡Áö ÀÌ»óÀÇ G-Protein Coupled Receptors(GPCR) Ÿ°Ù¿¡ ´ëÇÑ agonist¿Í antagonist¸¦ Á¦°øÇÕ´Ï´Ù. |
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Tocris |
Class A: Rhodopsin-like | ||
¢º CXC Chemokine Receptors | ||
Cat. No. | Product Name | Description |
Agonist | ¡¡ | ¡¡ |
4780 | VUF 11207 | Potent CXCR7 (ACKR3) agonist |
5668 | VUF 11222 | High affinity non-peptide CXCR3 agonist |
Antagonist | ¡¡ | ¡¡ |
3299 | AMD 3100 | Highly selective CXCR4 antagonist |
4179 | AMD 3465 | Potent, selective CXCR4 antagonist |
4487 | (±)-AMG 487 | CXCR3 antagonist; inhibits cell migration and metastasis |
5130 | CTCE 9908 | CXCR4 antagonist; antitumor |
4596 | IT1t | Potent CXCR4 antagonist |
¡¡ | ¡¡ | ¡¡ |
¢º Estrogen (GPER) Receptors | ||
Cat. No. | Product Name | Description |
Agonist | ¡¡ | ¡¡ |
3577 | G-1 | Potent and selective GPER agonist |
1047 | ICI 182,780 | High affinity GPER agonist |
Antagonist | ¡¡ | ¡¡ |
3678 | G-15 | High affinity and selective GPER antagonist |
¡¡ | ¡¡ | ¡¡ |
¢º Angiotensin Receptors | ||
Cat. No. | Product Name | Description |
Agonist | ¡¡ | ¡¡ |
1158 | Angiotensin II | Potent vasoconstrictor peptide |
5728 | EXP 3174 | Potent and selective AT1 antagonist |
Antagonist | ¡¡ | ¡¡ |
5798 | Irbesartan | Potent AT1 antagonist |
3798 | Losartan potassium | Selective, non-peptide AT1 antagonist |
1361 | PD 123319 | Potent, selective non-peptide AT2 antagonist |
¡¡ | ¡¡ | ¡¡ |
¢º Bradykinin Receptors | ||
Cat. No. | Product Name | Description |
Agonist | ¡¡ | ¡¡ |
3004 | Bradykinin | Endogenous agonist at bradykinin receptors (B2 > B1) |
Antagonist | ¡¡ | ¡¡ |
3014 | HOE 140 | Potent and selective B2 antagonist |
¡¡ | ¡¡ | ¡¡ |
¢º δ Opioid Receptor | ||
Cat. No. | Product Name | Description |
Agonist | ¡¡ | ¡¡ |
0764 | SNC 80 | Highly selective non-peptide δ agonist |
Antagonist | ¡¡ | ¡¡ |
0740 | Naltrindole | Selective non-peptide δ antagonist |
¡¡ | ¡¡ | ¡¡ |
¢º κ Opioid Receptor | ||
Cat. No. | Product Name | Description |
Agonist | ¡¡ | ¡¡ |
3195 | Dynorphin A | Endogenous κ agonist |
5519 | (-)-Pentazocine | κ agonist; antinociceptive |
0496 | (-)-U-50488 | Standard selective κ agonist; more active enantiomer of (±)-U-50488 (Cat. No. 0495) |
0495 | (±)-U-50488 | Standard selective κ agonist |
Antagonist | ¡¡ | ¡¡ |
0347 | nor-Binaltorphimine | Standard selective κ antagonist |
¡¡ | ¡¡ | ¡¡ |
¢º μ Opioid Receptor | ||
Cat. No. | Product Name | Description |
Agonist | ¡¡ | ¡¡ |
1171 | DAMGO | Selective μ agonist |
Antagonist | ¡¡ | ¡¡ |
1560 | CTAP | Selective and potent μ antagonist |
2601 | Cyprodime | Selective μ antagonist |
0926 | β-Funaltrexamine | Irreversible μ-selective antagonist |
¡¡ | ¡¡ | ¡¡ |
¢º Orexin Receptors | ||
Cat. No. | Product Name | Description |
Agonist | ¡¡ | ¡¡ |
1455 | Orexin A (human, rat, mouse) | Endogenous agonist at OX1 and OX2 |
2142 | [Ala11,D-Leu15]-Orexin B | Potent, selective OX2 receptor agonist |
1456 | Orexin B (human) | Endogenous agonist at OX1 and OX2 |
1457 | Orexin B (mouse) | Endogenous agonist at OX1 and OX2 |
Antagonist | ¡¡ | ¡¡ |
4983 | ACT 335827 | Potent and selective OX1 antagonist |
5319 | ACT 462206 | Potent, dual orexin receptor antagonist |
4558 | EMPA | Highly potent and selective OX2 antagonist; brain penetrant |
5645 | IPSU | OX2 receptor antagonist; orally bioavailable and brain penetrant |
4317 | JNJ 10397049 | Selective OX2 receptor antagonist |
¡¡ | ¡¡ | ¡¡ |
¢º Ghrelin Receptor | ||
Cat. No. | Product Name | Description |
Agonist | ¡¡ | ¡¡ |
1463 | Ghrelin (human) | Endogenous ghrelin receptor agonist |
1465 | Ghrelin (rat) | Endogenous ghrelin receptor agonist |
5272 | MK 0677 | High affinity ghrelin receptor agonist |
Antagonist | ¡¡ | ¡¡ |
1922 | [D-Lys3]-GHRP-6 | Ghrelin receptor antagonist |
3959 | YIL 781 | Ghrelin receptor (GHS-R1a) antagonist |
¡¡ | ¡¡ | ¡¡ |
¢º Motilin Receptor | ||
Cat. No. | Product Name | Description |
Agonist | ¡¡ | ¡¡ |
2264 | Motilin (human, porcine) | Endogenous motilin receptor agonist |
Antagonist | ¡¡ | ¡¡ |
5074 | ANQ 11125 | Selective motilin receptor antagonist |
4934 | MA 2029 | Potent and selective motilin receptor antagonist; orally active |
¡¡ | ¡¡ | ¡¡ |
¢º Dopamine D1/D5 Receptors | ||
Cat. No. | Product Name | Description |
Agonist | ¡¡ | ¡¡ |
1701 | A 77636 | Potent, selective D1-like agonist; orally active |
0884 | Dihydrexidine | Selective D1-like agonist |
0922 | SKF 38393 | Selective D1-like agonist |
1447 | SKF 81297 | D1 agonist |
2074 | SKF 83959 | D1-like partial agonist |
Antagonist | ¡¡ | ¡¡ |
0925 | SCH 23390 | Standard selective D1-like antagonist; also 5-HT2C and 5-HT1C agonist |
2299 | SCH 39166 | High affinity D1/D5 antagonist |
1586 | SKF 83566 | Potent, selective D1-like antagonist |
¡¡ | ¡¡ | ¡¡ |
¢º Dopamine D2/D3/D4 Receptors | ||
Cat. No. | Product Name | Description |
Agonist | ¡¡ | ¡¡ |
4552 | A 412997 | Selective D4 agonist |
1243 | (+)-PD 128907 | D3 agonist (D3 ≥ D2 > D4) |
1065 | PD 168077 | High affinity, selective D4 agonist |
2773 | Sumanirole | D2-selective agonist |
Antagonist | ¡¡ | ¡¡ |
1847 | Eticlopride | Selective D2/D3 antagonist |
1003 | L-741,626 | High affinity D2 antagonist |
1004 | L-741,742 | Highly selective D4 antagonist |
1002 | L-745,870 | Highly selective D4 antagonist |
4207 | SB 277011A | Selective D3 antagonist |
¡¡ | ¡¡ | ¡¡ |
¢º Histamine Receptors | ||
Cat. No. | Product Name | Description |
Agonist | ¡¡ | ¡¡ |
0646 | HTMT | H1 / H2 agonist |
0569 | (R)-(-)-α-Methylhistamine | Potent, standard H3 agonist |
2342 | 4-Methylhistamine | Selective, high affinity H4 agonist |
2478 | 2-Pyridylethylamine | H1 receptor agonist |
Antagonist | ¡¡ | ¡¡ |
3489 | Astemizole | Orally active, potent H1 antagonist; also KV11.1 (hERG) channel blocker |
3743 | BF 2649 | H3 receptor inverse agonist/antagonist |
0508 | Doxepin | Highly potent H1 antagonist; also binds to H4 receptor |
4021 | JNJ 7777120 | Selective H4 receptor antagonist |
0660 | Mepyramine | Selective H1 inverse agonist |
1070 | Zolantidine | Potent, centrally active H2 antagonist |
¡¡ | ¡¡ | ¡¡ |
Class B: Secretin-like | ||
¢º Glucagon Receptor | ||
Cat. No. | Product Name | Description |
Antagonist | ¡¡ | ¡¡ |
2216 | des-His1-[Glu9]-Glucagon (1-29) | Glucagon receptor antagonist |
2311 | L-168,049 | Potent, human glucagon receptor antagonist; orally active |
Other | ¡¡ | ¡¡ |
2094 | Oxyntomodulin | Endogenous gut peptide; modulates feeding and metabolism |
¡¡ | ¡¡ | ¡¡ |
¢º Glucagon-like Peptide Receptors | ||
Cat. No. | Product Name | Description |
Agonist | ¡¡ | ¡¡ |
1933 | Exendin-4 | Potent GLP-1 receptor agonist |
2082 | Glucagon-like peptide 1 (7-36) (human, rat) |
Potent insulinotropic peptide |
5374 | GLP-1 (7-37) | Endogenous bioactive GLP-1 receptor ligand |
Antagonist | ¡¡ | ¡¡ |
2081 | Exendin-3 (9-39) | Potent GLP-1 receptor antagonist |
3266 | GLP-1 (9-36) | Metabolite of GLP-1-(7-36) (Cat. No. 2082) |
Modulators | ¡¡ | ¡¡ |
4778 | BETP | Positive allosteric modulator of GLP-1 receptors |
¡¡ | ¡¡ | ¡¡ |
¢º Parathyroid Hormone (PTH) Receptors | ||
Cat. No. | Product Name | Description |
Agonist | ¡¡ | ¡¡ |
5487 | DPC AJ1951 | Potent PTH receptor agonist |
3011 | Parathyroid Hormone (1-43) (hunan) | PTH receptor agonist |
¡¡ | ¡¡ | ¡¡ |
Class C: Glutamate | ||
¢º GABAB Receptor | ||
Cat. No. | Product Name | Description |
Agonist | ¡¡ | ¡¡ |
0796 | (R)-Baclofen | Selective GABAB agonist; active enantiomer of (RS)-Baclofen |
3400 | RuBi-GABA | Caged GABA; excitable by visible wavelength |
Antagonist | ¡¡ | ¡¡ |
1245 | CGP 35348 | Brain penetrant, selective GABAB antagonist |
1246 | CGP 52432 | Potent, selective GABAB antagonist |
1088 | CGP 54626 | Potent, selective GABAB antagonist |
1248 | CGP 55845 | Potent, selective GABAB antagonist |
0984 | SCH 50911 | Selective, competitive, orally active GABAB antagonist |
Modulators | ¡¡ | ¡¡ |
1513 | CGP 7930 | Positive modulator at GABAB receptors |
¡¡ | ¡¡ | ¡¡ |
¢º Glutamate (Metabotropic) Receptors | ||
Cat. No. | Product Name | Description |
Agonist | ¡¡ | ¡¡ |
0187 | (±)-trans-ACPD | Group I/group II mGlu agonist |
1049 | CHPG | mGlu5 selective agonist |
3695 | CHPG Sodium salt | Selective mGlu5 agonist; sodium salt of CHPG |
0342 | (RS)-3,5-DHPG | Selective group I mGlu agonist |
0805 | (S)-3,5-DHPG | Selective group I mGlu agonist; active enantiomer of 3,5-DHPG |
0188 | L-Quisqualic acid | Group I mGlu agonist; also AMPA receptor agonist |
Antagonist | ¡¡ | ¡¡ |
5614 | AZD 2066 | mGlu5 antagonist; orally bioavailable and brain penetrant |
2501 | Bay 36-7620 | Non-competitive mGlu1 antagonist with inverse agonist activity |
0323 | (S)-4-Carboxyphenylglycine | Competitive group I mGlu antagonist/weak group II agonist |
1028 | CPCCOEt | Selective non-competitive mGlu1 receptor antagonist |
2333 | JNJ 16259685 | Highly potent, mGlu1-selective non-competitive antagonist |
1237 | LY 367385 | Selective mGlu1a antagonist |
Modulators | ¡¡ | ¡¡ |
¡¡ | ¡¡ | ¡¡ |
5322 | VU 0409106 | Potent and selective negative allosteric modulator at mGlu5 |
¡¡ | ¡¡ | ¡¡ |
GPCR Signaling | ||
¢º Adenylyl Cyclase | ||
Cat. No. | Product Name | Description |
Activators | ¡¡ | ¡¡ |
1099 | Forskolin | Adenylyl cyclase activator |
1603 | NKH 477 | Water-soluble adenylyl cyclase activator |
Inhibitors | ¡¡ | ¡¡ |
1435 | SQ 22536 | Adenylyl cyclase inhibitor |
¡¡ | ¡¡ | ¡¡ |
¢º cAMP | ||
Cat. No. | Product Name | Description |
Others | ¡¡ | ¡¡ |
5255 | 6-Bnz-cAMP sodium salt | Cell permeable cAMP analog |
1140 | 8-Bromo-cAMP, sodium salt | Cell-permeable cAMP analog |
1337 | cAMPS | cAMP antagonist |
1333 | cAMPS-Sp | Cell-permeable cAMP analog |
1141 | Dibutyryl-cAMP, sodium salt | Cell-permeable cAMP analog |
¡¡ | ¡¡ | ¡¡ |
¢º Phospholipases | ||
Cat. No. | Product Name | Description |
Inhibitors | ¡¡ | ¡¡ |
1437 | D609 | Selective PC-PLC inhibitor |
3022 | Edelfosine | Selective PI-PLC inhibitor; also PAF receptor agonist |
3600 | FIPI | Phospholipase D inhibitor |
1268 | U 73122 | Phospholipase C inhibitor |
3575 | VU 0155069 | Potent and selective PLD1 inhibitor |
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