G Protein Effectors and Antagonists

C3A Receptor Agonist
A G protein-coupled receptor protein involved in the complement system.
Katalog # CAS Nummer Summenformel Menge
sc-214644 944997-60-8 C₂₇H₃₅N₃O₂ 1 mg/5 mg
CID 2745687
Katalog # CAS Nummer Summenformel Menge
sc-362725 264233-05-8 C₁₇H₁₉F₂N₅O₂S 10 mg/50 mg
Compound 48/80 trihydrochloride
Oligomeric mixture of condensation products of N-methyl-p-methoxyphenethylamine and formaldehyde. Activates G proteins by a mechanism analogous to that of mastoparan.
Katalog # CAS Nummer Summenformel Menge
sc-200736 94724-12-6 C₃₂H₄₆N₃O₃ ·3HCl 100 mg/500 mg
Dimethyl-W84 dibromide
Very potent allosteric modulator of muscarinic receptors, selective for M2-receptors. Retards the dissociation of the antagonist N-methylscopolamine. pKA=7.08, p(αKA)=6.75, pEC5₅₀,diss=6.77.
Katalog # CAS Nummer Summenformel Menge
sc-202140 402475-33-6 C₃₄H₄₈Br₂N₄O₄ 5 mg
EHT 1864
Has been reported to be an inhibitor of Rac family GTPases via guanine nucleotide displacement. This compound has also been shown to modulate amyloid precursor protein (APP) processing which blocks Aβ 40 and Aβ 42 production.
Katalog # CAS Nummer Summenformel Menge
sc-361175 754240-09-0 C₂₅H₂₇F₃N₂O₄S•2HCl 10 mg/50 mg
FIPI
Isoforms of phospholipase D (PLD) cleave the head group from phospholipids, releasing the second messenger phosphatidic acid (PA), which can produce changes in Ras activation, cell spreading, stress fiber formation, chemotaxis, and membrane vesicle trafficking. FIPI is a derivative of halopemide which potently inhibits both PLD1 (IC50 = 25 nM) and PLD2 (IC50 = 20 nM). It also prevents PLD regulation of F-actin cytoskeleton reorganization, cell spreading, and chemotaxis. FIPI has good pharmacokinetic parameters in rats, with a half-life greater than five hours, a Cmax that, at 363 nM, is greater than 10-fold the IC50 versus PLD2, and bioavailability of 18%
Katalog # CAS Nummer Summenformel Menge
sc-294594 939055-18-2 C₂₃H₂₄FN₅O₂ 1 mg/5 mg
GPR30 Agonist, G-1
A cell-permeable, nonsteroidal, dihydroquinoline compound that acts as a high-affinity agonist for GPR30, the G protein-coupled transmembrane estrogen receptor in ER. It specifically competes with estrogen-binding to GPR30 (Ki = 11 nM), but not to the classical nuclear-residing estrogen receptors, ERα and ERβ (no significant binding upto 1 µM).
Katalog # CAS Nummer Summenformel Menge
sc-221685 881639-98-1 C₂₁H₁₈BrNO₃ 5 mg
Guanosine 5′-O-(2-Thiodiphosphate), Trilithium Salt
Cell impermeable, non-hydrolyzable analog of guanosine 5'-O-diphosphate (GDP) that competitively inhibits G-protein activation by GTP and GTP analogs.
Katalog # CAS Nummer Summenformel Menge
sc-295029 97952-36-8 C₁₀H₁₂Li₃N₅O₁₀P₂S 1 mg/5 mg
GW 848687X
Four G protein-coupled receptors, EP1-4, initiate cellular signaling in response to prostaglandin PGE2. The receptor EP1 acts via Gαq to evoke diverse effects, including renal vasoconstriction, bronchoconstriction, hyperalgesia, allodynia, gastric protection, hyperthermia, and sleep inhibition. GW 848687X is a potent and selective EP1 receptor antagonist (IC50 = 2. nM). It has >400-fold selectivity for EP1 relative to the other EP receptor subtypes, the PGD2 receptor, DP1, and the prostacyclin receptor, IP. GW 848687X has 30-fold selectivity over the thromboxane A2 receptor, TP, acting as a functional antagonist at this receptor at higher levels. Its actions against the FP and CRTH2/DP2 receptors have not been characterized. In vivo, GW 848687X has an excellent oral pharmacokinetic profile, with oral bioavailability at 54% in rats and 53% in dogs with a half-life of two hours in both species. In a rat model of chronic inflammatory joint pain, GW 848687X shows complete anti-hyperalgesic activity.
Katalog # CAS Nummer Summenformel Menge
sc-295034 612831-24-0 C₂₄H₁₈ClF₂NO₃ 500 µg/1 mg
Isotetrandrine
Isotetrandrine is a biscoclaurine alkaloid inhibitor of G protein activation of PLA2 but not PLC or PLD.
Katalog # CAS Nummer Summenformel Menge
sc-200869 477-57-6 C₃₈H₄₂N₂O₆ 1 mg/5 mg
Mastoparan (Vespula lewisii)
Shown to be capable of directly activating G proteins by a mechanism analogous to that of G protein-coupled receptors. Also found to stimulate insulin release by pancreatic islets.
Katalog # CAS Nummer Summenformel Menge
sc-200831 72093-21-1 C₇₀H₁₃₁N₁₉O₁₅ 1 mg
Melittin
Shown to cause apoptosis via induction of reactive oxygen species production in cells. Also reported to inhibit activator protein-1 as well as NF-κB.
Katalog # CAS Nummer Summenformel Menge
sc-200868 37231-28-0 C₁₃₁H₂₂₉N₃₉O₃₁ 500 µg
Metastin (45-54)
This is a decapeptide with C-terminally amidated LRF-motif which acts as a potent and selective agonist of AXOR12 and hOT7T175 (a novel human G-protein-coupled receptors). It induces an increase in intracellular Ca²⁺ levels in CHO/h175 and CHO/AXOR12:Gqi5 cells and exhibits about 8-fold higher receptor binding affinity (Ki = 42 pM) compared to Metastin.
Katalog # CAS Nummer Summenformel Menge
sc-221883 374675-21-5 C₆₃H₈₃N₁₇O₁₄ 1 mg
N-Formyl-Met-Leu-Phe
Katalog # CAS Nummer Summenformel Menge
sc-358988 59880-97-6 C₂₁H₃₁N₃O₅S 5 mg/10 mg
N2-[[5-(Diphenylmethyl)-2-furanyl]carbonyl]-L-Arginine hydrate
A C3a receptor antagonist where the complement component 3a receptor is a G protein-coupled receptor protein involved in the complement system.
Katalog # CAS Nummer Summenformel Menge
sc-215516 945254-73-9 (anhydrous) C₂₄H₂₆N₄O₄•xH₂O 1 mg
PF9 tetrasodium salt
Katalog # CAS Nummer Summenformel Menge
sc-362783 851265-78-6 C₁₈H₁₆N₅Na₄O₁₃P₃ 1 mg
Polistes Mastoparan
This product is a peptide found in wasp venom. It binds to and inhibits calmodulin, a calcium binding protein found in eukaryotic cells.
Katalog # CAS Nummer Summenformel Menge
sc-200832 74129-19-4 C₇₇H₁₂₇N₂₁O₁₈ 1 mg
TC-O 9311
Katalog # CAS Nummer Summenformel Menge
sc-362802 444932-31-4 C₂₀H₁₉N₃O₄ 10 mg/50 mg
W146 trifluoroacetate salt
Sphingosine-1-phosphate (S1P) is a bioactive lipid that exhibits a broad spectrum of biological activities including cell proliferation, survival, migration, cytoskeletal organization, and morphogenesis. It exerts its activity by binding to five distinct G protein-coupled receptors, S1P1/EDG-1, S1P2/EDG-5, S1P3/EDG-3, S1P4/EDG-6, and S1P5/EDG-8. W146 is a S1P1 receptor antagonist that exhibits a Ki value of 77 nM for the human receptor in a GTP-γS binding assay with equipotency at the murine S1P1 receptor (2a = W146; 2b = W140 in supplemental material). No agonist or antagonist activity was observed at 10 µM W146 at S1P2, S1P3, or S1P5 receptors. W146 is active in vivo causing skin capillary leakage in murine lung and skin as well as inhibition of S1P1 agonist-induced lymphocyte sequestration. The half-life of W146 in rat blood is 73 minutes.
Katalog # CAS Nummer Summenformel Menge
sc-296700 n.n. C₁₆H₂₇N₂O₄P•C₂F₃HO₂ 500 µg/1 mg
WZ811
The CXC chemokine receptor-4 (CXCR4) is a G protein-coupled receptor that is specific for stromal cell-derived factor-1 (SDF-1, CXCL12). Activation of CXCR4 promotes homing of hematopoietic stem cells, chemotaxis and quiescence of lymphocytes, and growth and metastasis of certain cancer cell types. Moreover, CXCR4 on CD4+ T-cells is used by CXCR4-selective HIV forms as a gateway for T-cell infection. WZ811 is a potent inhibitor of binding of an SDF-1 peptide mimic to CXCR4 (EC50 = 0. nM). It prevents SDF-1/CXCL12-mediated modulation of cAMP (EC50 = 1. nM) in cells and blocks SDF-1-induced Matrigel invasion by MDA-MB-231 human breast adenocarcinoma cells (EC50 = 5. nM). The effectiveness of WZ811 in animals remains to be elucidated.
Katalog # CAS Nummer Summenformel Menge
sc-296701 55778-02-4 n.n. 1 mg/5 mg
YS121
Microsomal prostaglandin E2 synthase-1 (mPGES-1), with cyclooxygenase-2 (COX-2), synthesizes PGE2, which is directly involved in signaling during inflammation, fever, and pain. 5-Lipoxygenase (5-LO) initiates the synthesis of leukotrienes (LTs), which are pro-inflammatory mediators. YS121 is a dual inhibitor of mPGES-1 (IC50 = 3.9 μM) and 5-LO (IC50 = 4. μM). It effectively inhibits PGE2 and LT synthesis in both cell free and intact cell assays. Moreover, YS121 (1. mg/kg, intraperitoneal) reduced pleural levels of PGE2 and LTB4 while blocking exudate formation and leukocyte infiltration in carrageenan-induced rat pleurisy. YS121 has minor effects on COX-1 and COX-2, inhibiting these enzymes 24.8% and 38%, respectively, at 10 μM
Katalog # CAS Nummer Summenformel Menge
sc-296707 916482-17-2 C₂₀H₂₆ClN₃O₂S 1 mg/5 mg