16,16-Dimethyl Prostaglandin E2 - CAS 39746-25-3
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
Molecular Weight:
Prostaglandin Receptor
16,16-Dimethyl Prostaglandin E2, a prostaglandin E2 derivative, could induce an increase in hematopoietic stem cell (HSC) numbers in mouse model.
≥98% by HPLC
Colourless Liquid
(5Z,11α,13E,15R)-11,15-Dihydroxy-16,16-dimethyl-9-oxo-prosta-5,13-dien-1oic acid
Canonical SMILES:
1.Peripheral prostaglandin E2 prolongs the sensitization of nociceptive dorsal root ganglion neurons possibly by facilitating the synthesis and anterograde axonal trafficking of EP4 receptors.
St-Jacques B1, Ma W2. Exp Neurol. 2014 Nov;261:354-66. doi: 10.1016/j.expneurol.2014.05.028. Epub 2014 Jun 5.
Prostaglandin E2 (PGE2), a well-known pain mediator enriched in inflamed tissues, plays a pivotal role in the genesis of chronic pain conditions such as inflammatory and neuropathic pain. PGE2-prolonged sensitization of nociceptive dorsal root ganglion (DRG) neurons (nociceptors) may contribute to the transition from acute to chronic pain. However, the underlying cellular mechanisms are poorly understood. In this study, we tested the hypothesis that facilitating synthesis and anterograde axonal trafficking of EP receptors contribute to PGE2-prolonged nociceptor sensitization. Intraplantar (i.pl.) injection of a stabilized PGE2 analog, 16,16 dimethyl PGE2 (dmPGE2), in a dose- and time-dependent manner, not only elicited primary tactile allodynia which lasted for 1d, but also prolonged tactile allodynia evoked by a subsequent i.pl. injection of dmPGE2 from 1d to 4d. Moreover, the duration of tactile allodynia was progressively prolonged following multiple sequential i.
2.Chronic prostaglandin E2 treatment induces the synthesis of the pain-related peptide substance P and calcitonin gene-related peptide in cultured sensory ganglion explants.
Ma W1. J Neurochem. 2010 Oct;115(2):363-72. doi: 10.1111/j.1471-4159.2010.06927.x. Epub 2010 Aug 25.
Prostaglandin E2 (PGE2) is a well known pain and pro-inflammatory mediator abundantly produced in inflamed tissue. It causes pain by directly exciting nociceptive primary sensory neurons (nociceptors) and indirectly stimulating the release of pain-related peptide substance P (SP) and calcitonin gene-related peptide (CGRP). In an ex vivo culture of sensory ganglion explants, we tested the hypothesis that PGE2 could induce the synthesis of SP and CGRP in nociceptors. A stabilized PGE2 analog, 16,16-dimethyl PGE2, in a concentration- and time-dependent manner, significantly increased mRNA and peptide levels of SP and CGRP. The agonists of EP1 and EP4 receptors also significantly increased SP and CGRP levels. Moreover, 16,16-dimethyl PGE2-induced SP and CGRP were blocked by EP1 and EP4 antagonists as well as the inhibitors of both protein kinase A and protein kinase C. Nerve growth factor was partially involved in PGE2-induced SP and CGRP synthesis.
3.Endogenous prostaglandin E2 accelerates healing of indomethacin-induced small intestinal lesions through upregulation of vascular endothelial growth factor expression by activation of EP4 receptors.
Takeuchi K1, Tanigami M, Amagase K, Ochi A, Okuda S, Hatazawa R. J Gastroenterol Hepatol. 2010 May;25 Suppl 1:S67-74. doi: 10.1111/j.1440-1746.2010.06222.x.
BACKGROUND AND AIMS: The effects of an EP4 agonist/antagonist on the healing of lesions produced by indomethacin in the small intestine were examined in rats, especially in relation to the expression of vascular endothelial growth factor (VEGF) and angiogenesis.
4.Autocrine prostaglandin E2 signaling promotes tumor cell survival and proliferation in childhood neuroblastoma.
Rasmuson A1, Kock A, Fuskevåg OM, Kruspig B, Simón-Santamaría J, Gogvadze V, Johnsen JI, Kogner P, Sveinbjörnsson B. PLoS One. 2012;7(1):e29331. doi: 10.1371/journal.pone.0029331. Epub 2012 Jan 19.
BACKGROUND: Prostaglandin E(2) (PGE(2)) is an important mediator in tumor-promoting inflammation. High expression of cyclooxygenase-2 (COX-2) has been detected in the embryonic childhood tumor neuroblastoma, and treatment with COX inhibitors significantly reduces tumor growth. Here, we have investigated the significance of a high COX-2 expression in neuroblastoma by analysis of PGE(2) production, the expression pattern and localization of PGE(2) receptors and intracellular signal transduction pathways activated by PGE(2).
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Prostaglandin Receptor Products

CAS 439288-66-1 GW 627368X

GW 627368X
(CAS: 439288-66-1)

GW 627368X is a potent and selective competitive antagonist of the EP4 receptor with additional human TP receptor affinity (Ki values of 100 nM and 158 nM, resp...

ONO 8711 dicyclohexyl amine salt

ONO 8711 dicyclohexyl amine salt is a selective and competitive prostaglandin E (PGE) receptor EP1 antagonist with chemopreventive activity. It suppresses tumor...

CAS 892549-43-8 Mf-63

(CAS: 892549-43-8)

Mf-63 is a selective Microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitor. Its IC50 value is 0.9 nM and 1.3 nM for pig mPGES-1 and human mPGES-1 enzyme, r...

(CAS: 1078166-57-0)

PF-04418948 is a potent and selective prostaglandin EP₂ receptor antagonist with IC50 of 16 nM. Phase 1. PF-04418948 antagonizes the effects of butaprost and PG...

CAS 872365-14-5 Fevipiprant

(CAS: 872365-14-5)

Fevipipran is a reversible competitive CRTh2 antagonist with IC50 value of 0.44 nM for inhibition of PGD2-induced eosinophil shape change in human whole blood. ...

CAS 572874-50-1 MK 0524 sodium salt

MK 0524 sodium salt
(CAS: 572874-50-1)

MK 0524 sodium salt is a potent and selective prostaglandin D2 (PGD2) receptor 1 (DP1) antagonist with Ki values to be 0.57 nM and 750 nM for DP1 and DP2 recept...

CAS 157283-68-6 Travoprost

(CAS: 157283-68-6)

Travoprost is a potent and selective FP prostaglandin receptor agonist used for the treatment of glaucoma.

(CAS: 165538-40-9)

Terutroban is a potent, orally active antagonist of the thromboxane/prostaglandin A2(TP) receptor (IC50 = 16.4 nM). In guinea pigs it also inhibits U 46619 indu...

Chemical Structure

CAS 39746-25-3 16,16-Dimethyl Prostaglandin E2

Quick Inquiry

Verification code

Featured Items