Date published: 2026-5-30

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Gα i-1 Activators

The term Gα i-1 activators encompasses a diverse group of chemicals that modulate the activity of the G protein subunit Gα i-1, a key player in intracellular signaling cascades. Gα i-1 is a member of the inhibitory G protein family, and its activation or inhibition regulates downstream signaling pathways in response to various extracellular signals. Here, we explore the mechanisms by which these activators directly or indirectly influence Gα i-1 and the physiological consequences of such modulation. Pertussis toxin, an exotoxin produced by Bordetella pertussis, is a direct inhibitor of Gα i proteins. It accomplishes this through ADP-ribosylation, preventing the interaction of Gα i-1 with receptors and disrupting downstream signaling pathways. On the other hand, mastoparan, a wasp venom peptide, directly activates Gα i-1 by promoting the exchange of GDP for GTP on the protein, facilitating downstream signaling cascades. Opioid analgesics, exemplified by fentanyl, indirectly modulate Gα i-1 activation. Fentanyl activates opioid receptors, leading to the inhibition of adenylyl cyclase and subsequent activation of Gα i-1. This indirect modulation is crucial for the analgesic effects of opioids.

Peptides such as bradykinin indirectly influence Gα i-1 by activating G protein-coupled receptors. Bradykinin binding induces Gα i-1 activation, leading to downstream effects on vasodilation, inflammation, and pain perception. Neurotransmitters like acetylcholine indirectly modulate Gα i-1 activation by stimulating muscarinic acetylcholine receptors, impacting heart rate and smooth muscle contraction. Lysophosphatidylcholine (LPC), a phospholipid, directly activates Gα i-1 through specific receptors, influencing cellular responses such as migration, proliferation, and inflammation. Alpha-2 adrenergic agonists, including clonidine and dexmedetomidine, indirectly modulate Gα i-1 activation.

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Mastoparan

72093-21-1sc-200831
1 mg
$99.00
(1)

A wasp venom peptide that activates G proteins. Mastoparan interacts with the lipid bilayer of cell membranes, facilitating G protein activation by promoting the exchange of GDP for GTP on Gα i-1. This direct activation enhances downstream signaling cascades associated with Gα i-1.

Carbachol

51-83-2sc-202092
sc-202092A
sc-202092C
sc-202092D
sc-202092B
sc-202092E
1 g
10 g
25 g
50 g
100 g
250 g
$122.00
$281.00
$388.00
$683.00
$1428.00
$3060.00
12
(2)

A cholinergic agonist that indirectly influences Gα i-1 activation. Carbachol stimulates muscarinic acetylcholine receptors, leading to the activation of Gα i proteins. This indirect activation plays a role in the regulation of various physiological processes, including smooth muscle contraction.

D-erythro-Sphingosine-1-phosphate

26993-30-6sc-201383
sc-201383D
sc-201383A
sc-201383B
sc-201383C
1 mg
2 mg
5 mg
10 mg
25 mg
$165.00
$322.00
$570.00
$907.00
$1727.00
7
(1)

A bioactive lipid that activates G protein-coupled receptors, including S1P receptors linked to Gα i proteins. S1P binding induces conformational changes in Gα i-1, leading to downstream signaling events. This direct activation plays a role in cellular processes such as cell migration and immune responses.

Lysophosphatidic Acid

325465-93-8sc-201053
sc-201053A
5 mg
25 mg
$98.00
$341.00
50
(3)

A phospholipid that activates G protein-coupled receptors, including LPA receptors coupled to Gα i proteins. LPA binding triggers Gα i-1 activation, leading to downstream signaling events involved in cell proliferation, survival, and migration. This direct activation contributes to the diverse effects of LPA.

Bradykinin

58-82-2sc-507311
5 mg
$110.00
(0)

A peptide that activates G protein-coupled receptors, including bradykinin receptors linked to Gα i proteins. Bradykinin binding induces Gα i-1 activation, leading to downstream signaling events involved in vasodilation, inflammation, and pain perception. This direct activation contributes to the diverse effects of bradykinin.

PGE1 (Prostaglandin E1)

745-65-3sc-201223
sc-201223A
1 mg
10 mg
$31.00
$145.00
16
(4)

A prostaglandin that activates G protein-coupled receptors, including certain prostanoid receptors coupled to Gα i proteins. PGE1 binding induces Gα i-1 activation, leading to downstream signaling events. This direct activation plays a role in smooth muscle relaxation and vasodilation, among other physiological responses.

L-α-Lysophosphatidylcholine (from egg yolk)

9008-30-4sc-473611
sc-473611A
sc-473611B
sc-473611C
25 mg
100 mg
500 mg
1 g
$87.00
$235.00
$607.00
$1102.00
1
(0)

A phospholipid that activates G protein-coupled receptors, including certain LPA receptors linked to Gα i proteins. LPC binding induces Gα i-1 activation, leading to downstream signaling events. This direct activation contributes to cellular responses such as migration, proliferation, and inflammation mediated by Gα i-1.