Treprostinil (diethanolamine salt)

Modify Date: 2024-01-04 20:39:42

Treprostinil (diethanolamine salt) structure	Common Name	Treprostinil (diethanolamine salt)
	CAS Number	830354-48-8	Molecular Weight	495.64900
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₂₇H₄₅NO₇	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of Treprostinil (diethanolamine salt)

Treprostinil (UT-15C) diethanolamine is a potent EP2, DP1 and IP agonist with Ki values of 3.6, 4.4, 32.1, 212, 826, 2505 and 4680 nM for EP2, DP1, IP, EP1, EP4, EP3 and FP, respectively. Treprostinil (UT-15C) diethanolamine increases upregulation of cAMP toward maintaining homeostasis within the vasculature. Treprostinil (UT-15C) diethanolamine can result in vasodilatation of human pulmonary arteries[1][2][3].

Name	2-[[(1R,2R,3aS,9aS)-2-hydroxy-1-[(3S)-3-hydroxyoctyl]-2,3,3a,4,9,9a-hexahydro-1H-cyclopenta[g]naphthalen-5-yl]oxy]acetic acid,2-(2-hydroxyethylamino)ethanol
Synonym	More Synonyms

Description	Treprostinil (UT-15C) diethanolamine is a potent EP2, DP1 and IP agonist with Ki values of 3.6, 4.4, 32.1, 212, 826, 2505 and 4680 nM for EP2, DP1, IP, EP1, EP4, EP3 and FP, respectively. Treprostinil (UT-15C) diethanolamine increases upregulation of cAMP toward maintaining homeostasis within the vasculature. Treprostinil (UT-15C) diethanolamine can result in vasodilatation of human pulmonary arteries[1][2][3].
Related Catalog	Research Areas >> Endocrinology Signaling Pathways >> GPCR/G Protein >> Prostaglandin Receptor
Target	DP/DP1:4.4 nM (Ki) IP:32.1 nM (Ki) EP1:212 nM (Ki) EP2:3.6 nM (Ki) EP3:826 nM (Ki) EP4:2505 nM (Ki) FP:4680 nM (Ki)
In Vitro	Treprostinil (UT-15C) diethanolamine (0.001-10,000 nM; 60 min; HEK293 cells) has high potency in activating DP1 and EP2 receptors as well as the IP receptor with EC50 values of 0.6 nM, 6.2 nM and 1.9 nM, respectively, 36-fold less active at the EP3 receptor, 95-fold less active at the EP4 and 150-fold less active at the EP1 site than at the IP receptor[1]. Treprostinil (UT-15C) diethanolamine (10 μM) increases cAMP accumulation in murine and human hematopoietic stem and progenitor cells (HSPCs) [2]. Treprostinil (UT-15C) diethanolamine (10 μM; 2-6 h; PC3 cells) enhances the action of SDF-1 via CXCR4[2].
In Vivo	Treprostinil (UT-15C) diethanolamine (0.15 mg/kg; i.h.; every 8 h; for 10 d; BALB/c mice) enhances the ability of HSPCs to repopulate the bone marrow and increases bone marrow reconstitution[2]. Treprostinil (UT-15C) diethanolamine (0.15 mg/kg; i.h.; every 8 h; for 10 d; BALB/c mice) increases survival of lethally irradiated recipient mice[2]. Treprostinil (UT-15C) diethanolamine (0.1 mg/kg; i.h.; for 24h; male lewis rats) inhibits the mRNA expression of TNF-α and IFN-γ and increases in IL-10 expression[3]. Animal Model: BALB/c mice[2] Dosage: 0.15 mg/kg Administration: Subcutaneous injection; every 8 hours; for 10 days Result: Increased survival of lethally irradiated recipient mice. Animal Model: Male lewis rats[3] Dosage: 0.1 mg/kg Administration: Subcutaneous injection; for 24 hours Result: Decreased the mRNA expression of TNF-α and IFN-γ and increased the expression of IL-10.
References	[1]. Whittle BJ, et, al. Binding and activity of the prostacyclin receptor (IP) agonists, treprostinil and iloprost, at human prostanoid receptors: treprostinil is a potent DP1 and EP2 agonist. Biochem Pharmacol. 2012 Jul 1;84(1):68-75. [2]. Kazemi Z, et, al. Repurposing Treprostinil for Enhancing Hematopoietic Progenitor Cell Transplantation. Mol Pharmacol. 2016 Jun;89(6):630-44. [3]. Ghonem N, et, al. Treprostinil, a prostacyclin analog, ameliorates ischemia-reperfusion injury in rat orthotopic liver transplantation. Am J Transplant. 2011 Nov;11(11):2508-16.

Molecular Formula	C₂₇H₄₅NO₇
Molecular Weight	495.64900
Exact Mass	495.32000
PSA	146.89000

dea

CAS#:111-42-2

Treprostinil

CAS#:81846-19-7

~80%

Treprostinil (d...

CAS#:830354-48-8

Literature: UNITED THERAPEUTICS CORPORATION Patent: US2009/163738 A1, 2009 ; Location in patent: Page/Page column 6-7 ;

Precursor 2
CAS#:111-42-2 dea CAS#:81846-19-7 Treprostinil
DownStream 1
CAS#:81846-19-7 Treprostinil

Treprostinil diethanolamine

TREPROSTINIL DIOLAMINE

UT-15C

treprostinil diethanolamine salt

Treprostinil (diethanolamine salt)

Use of Treprostinil (diethanolamine salt)

Names

Treprostinil (diethanolamine salt) Biological Activity

Chemical & Physical Properties

Synthetic Route

Precursor & DownStream

Synonyms