1. GPCR/G Protein
  2. Prostaglandin Receptor
  3. KMN-80

KMN-80 

Cat. No.: HY-118743
Handling Instructions

KMN-80, a derivative of PGE1 (HY-B0131), is a selective and potent agonist of EP4 receptor with an IC50 and a Ki of 3 nM and 2.35 nM, respectively. KMN-80 is against EP3 receptor with an IC50 of 1.4 μM and >10 μM for all other prostanoid receptors.

For research use only. We do not sell to patients.

KMN-80 Chemical Structure

KMN-80 Chemical Structure

CAS No. : 1628759-75-0

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Description

KMN-80, a derivative of PGE1 (HY-B0131), is a selective and potent agonist of EP4 receptor with an IC50 and a Ki of 3 nM and 2.35 nM, respectively. KMN-80 is against EP3 receptor with an IC50 of 1.4 μM and >10 μM for all other prostanoid receptors[1].

IC50 & Target[1]

EP4 Receptor

3 nM (IC50)

EP3 receptor

1.5 μM (IC50)

h-EP4

2.349 nM (Ki)

hEP3A Receptor

880 nM (Ki)

In Vitro

KMN-80 is tested for binding of EP4 receptor and for activation of the rat EP2 and EP4 receptors, exhibits a Ki of 1.11 nM for rat EP4 receptor, EC50 values of 2.66 nM and 0.17 nM for rat EP4 receptor cAMP levels and rat EP4 receptor CREB activation, respectively[1].
BMCs are isolated from young female rats are treated once at plating with varying doses of KMN-80 and ALP enzyme activity determined on day 9. KMN-80 (0-100 nM) shows ALP EC50 values significant different than those corresponding to PGE2 and PGE1, the EC50 values are 82.1 nM and 29.3 nM in activation of ALP enzyme activity in young female rat BMCs or old female or young male rat BMCs, respectively[1].
KMN-80has been shown to stimulate secreted alkaline phosphatase gene reporter activity in EP4-transfected HEK293 cells with an EC50 value of 0.19 nM, demonstrating >5,000 and 50,000-fold selectivity against EP2 and TP, respectively[2].
KMN-80 can induce the differentiation of bone marrow stem cells from both young and aged rats into osteoblasts in vitro (EC50s=20 and 153 nM, respectively) and exhibits favorable tolerability up to at least 10 μM, whereas the EP4 agonist L-902,688 is highly cytotoxic at similar concentrations in these cells[2].
KMN-80 binds to human EP receptor subtypes with Ki values of 880 nM and 2.349 nM for hEP3 and hEP4, respectively[2].

Molecular Weight

363.49

Formula

C₂₁H₃₃NO₄

CAS No.

1628759-75-0

SMILES

OC(CCCCCCN(C1=O)[[email protected]](CC1)/C=C/[[email protected]@H](O)[[email protected]@H](C)CC#CCC)=O

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

KMN-80KMN80KMN 80Prostaglandin ReceptorProstaglandin EBone MarrowOsteoblastic Differentiation ALPBMCEP4 receptorderivativePGE1Inhibitorinhibitorinhibit

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KMN-80
Cat. No.:
HY-118743
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