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MedKoo Cat#: 574354 | Name: ER-50891
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

ER-50891 is an antagonist of RARα receptors that displays selective affinity for RARα.

Chemical Structure

ER-50891
ER-50891
CAS#187400-85-7

Theoretical Analysis

MedKoo Cat#: 574354

Name: ER-50891

CAS#: 187400-85-7

Chemical Formula: C29H24N2O2

Exact Mass: 432.1838

Molecular Weight: 432.52

Elemental Analysis: C, 80.53; H, 5.59; N, 6.48; O, 7.40

Price and Availability

Size Price Availability Quantity
10mg USD 650.00 2 Weeks
50mg USD 2,050.00 2 Weeks
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Related CAS #
No Data
Synonym
ER-50891, ER50891, ER 50891
IUPAC/Chemical Name
4-(5-(8-isopropyl-4-phenylquinolin-2-yl)-1H-pyrrol-2-yl)benzoic acid
InChi Key
LSGNKLDHMQVTEK-UHFFFAOYSA-N
InChi Code
InChI=1S/C29H24N2O2/c1-18(2)22-9-6-10-23-24(19-7-4-3-5-8-19)17-27(31-28(22)23)26-16-15-25(30-26)20-11-13-21(14-12-20)29(32)33/h3-18,30H,1-2H3,(H,32,33)
SMILES Code
CC(C)C1=C2C(C(C3=CC=CC=C3)=CC(C4=CC=C(C5=CC=C(C(O)=O)C=C5)N4)=N2)=CC=C1
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Selective RARα antagonist.
In vitro activity:
From 0.5 to 1.5 µM, ER-50891 significantly antagonized the inhibitive effect of ATRA and dose-dependently increased the total cell metabolic activity of preosteoblasts (Supplementary Figure 1A). ER-50891 of all the selected concentrations resulted in a significantly higher level of DNA content than the group of ATRA alone, which reached a similar level as the control (Supplementary Figure 1B). ATRA decreased total protein content to 48.0% of the control group. In contrast, ER-50891 dose-dependently increase the total protein content of preosteoblasts (Figure 3A) with protein content recovered to 80.6% of the control group. ATRA increased ALP activity by 2.5 fold, which could be dose-dependently inhibited by ER-50891 (Figure 3B). ATRA decreased OCN expression to 23.4% of the control, which could be dose-dependently relieved by ER-50891. ER-50891 at 2 and 3 µM almost completely rescued the OCN expression (Figure 3C). Reference: Drug Des Devel Ther. 2020; 14: 297–308. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6985983/
In vivo activity:
TBD
Solvent mg/mL mM
Solubility
DMSO 43.3 100.00
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 432.52 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Wang S, Bi W, Liu Y, Cheng J, Sun W, Wu G, Xu X. The Antagonist of Retinoic Acid Receptor α, ER-50891 Antagonizes the Inhibitive Effect of All-Trans Retinoic Acid and Rescues Bone Morphogenetic Protein 2-Induced Osteoblastogenic Differentiation. Drug Des Devel Ther. 2020 Jan 22;14:297-308. doi: 10.2147/DDDT.S215786. PMID: 32158187; PMCID: PMC6985983. 2. Hou PS, Huang WC, Chiang W, Lin WC, Chien CL. Impaired neural differentiation potency by retinoic acid receptor-α pathway defect in induced pluripotent stem cells. Cell Reprogram. 2014 Dec;16(6):467-76. doi: 10.1089/cell.2014.0029. Epub 2014 Nov 3. PMID: 25364979; PMCID: PMC4245853.
In vitro protocol:
1. Wang S, Bi W, Liu Y, Cheng J, Sun W, Wu G, Xu X. The Antagonist of Retinoic Acid Receptor α, ER-50891 Antagonizes the Inhibitive Effect of All-Trans Retinoic Acid and Rescues Bone Morphogenetic Protein 2-Induced Osteoblastogenic Differentiation. Drug Des Devel Ther. 2020 Jan 22;14:297-308. doi: 10.2147/DDDT.S215786. PMID: 32158187; PMCID: PMC6985983. 2. Hou PS, Huang WC, Chiang W, Lin WC, Chien CL. Impaired neural differentiation potency by retinoic acid receptor-α pathway defect in induced pluripotent stem cells. Cell Reprogram. 2014 Dec;16(6):467-76. doi: 10.1089/cell.2014.0029. Epub 2014 Nov 3. PMID: 25364979; PMCID: PMC4245853.
In vivo protocol:
TBD
1. Kikuchi et al (2001) Syntheses and evaluation of quinoline derivatives as novel retinoic acid receptor α antagonists. Bioorg.Med.Chem.Lett. 11 1215 PMID: 11354380 2. Ren et al (2005) Impaired retinoic acid (RA) signal leads to RARβ2 epigenetic silencing and RA resistance. Mol.Cell.Biol. 25 10591 PMID: 16287870 3. Somenzi et al (2007) Disruption of retinoic acid receptor alpha reveals the growth promoter face of retinoic acid. PLoS ONE 9 e836 PMID: 17786207