| 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 |
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