• Home
  • About us
  • Log-In
  • Join Us
  • Sitemap
  • Recruit
ǰ/ Q&A
ֹ
Խ
ڷû
ڷ
Ŭ
A/S
Ŭ ȸ
 ǰȳ  鿪   Cell Signaling  GPCR Product

GPCR Inhibitor & Activator

 õ class 450 ̻ G-Protein Coupled Receptors(GPCR) Ÿٿ agonist antagonist մϴ.

Tocris
ǰ ϱ
μϱ

Ư¡

Class A: Rhodopsin-like
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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

GPCR μ