[CAS NO. 187269-40-5] Bimosiamose

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PRODUCTS SPECIFICATIONS [187269-40-5]

Catalog

HY-106139

Brand

MCE

CAS

187269-40-5

DESCRIPTION [187269-40-5]

Overview

MDL	-
Molecular Weight	862.91
Molecular Formula	C46H54O16
SMILES	OC[C@H]([C@@H](O)[C@H](O)[C@@H]1O)O[C@@H]1OC(C=C2)=C(C3=CC(CC(O)=O)=CC=C3)C=C2CCCCCCC(C=C4)=CC(C5=CC(CC(O)=O)=CC=C5)=C4O[C@H]6O[C@@H]([C@@H](O)[C@H](O)[C@@H]6O)CO

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

2 Publications Citing Use of MCE

Summary

Bimosiamose (TBC-1269) is a nonoligosaccharide pan- selectin antagonist with IC ₅₀ s of 88 μM, 20 μM, and 86 μM for E-selectin , P-selectin , and L-selectin , respectively. Bimosiamose has anti-inflammatory effects ^[1] .

IC50 & Target

IC50: 88 μM (E-selectin), 20 μM (P-selectin), 86 μM (L-selectin) ^[1]

In Vitro

Bimosiamose (TBC-1269) operates by inhibiting neutrophil recruitment to the site of inflammation through blocking the initial rolling phase of recruitment. Bimosiamose (TBC-1269) inhibits cell recruitment and does not possess any cytotoxic effect on neutrophils ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Bimosiamose (TBC-1269; 25 mg/kg; intravenous injection; Sprague-Dawley rats) treatment shows a significant increase in survival. Best overall survival, 70%, is observed when TBC-1269 is administered 15 minutes before reperfusion, and also shows a marked decrease in liver enzyme levels at 6 hours after reperfusion. Neutrophil migration is also significantly ameliorated (81%). The histologic damage scores is also improved ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Sprague-Dawley rats (200-225g) with ischemia and reperfusion (I/R) ^[1]
Dosage:	25 mg/kg
Administration:	Intravenous injection
Result:	Showed a significant increase in survival compared with controls.

Clinical Trial

NCT Number	Sponsor	Condition	Phase
NCT00823693	Revotar Biopharmaceuticals AG	Psoriasis	Phase 2
NCT00962481	Revotar Biopharmaceuticals AG	Chronic Obstructive Pulmonary Disease (COPD)	Phase 2
NCT01108913	Revotar Biopharmaceuticals AG	Chronic Obstructive Pulmonary Disease	Phase 2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL ( 115.89 mM ; Need ultrasonic)

0.1 M NaOH : 25 mg/mL ( 28.97 mM ; ultrasonic and adjust pH to 10 with NaOH)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.1589 mL	5.7943 mL	11.5887 mL
5 mM	0.2318 mL	1.1589 mL	2.3177 mL
10 mM	0.1159 mL	0.5794 mL	1.1589 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 5% DMSO >> 40% PEG300 >> 5% Tween-80 >> 50% saline

Solubility: ≥ 2.5 mg/mL (2.90 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[1] Palma-Vargas JM, et al. Small-molecule selectin inhibitor protects against liver inflammatory response after ischemia and reperfusion. J Am Coll Surg. 1997 Oct;185(4):365-72.

Synonyms

[1,1′-Biphenyl]-3-acetic acid, 3′,3′′′-(1,6-hexanediyl)bis[6′-(α-D-mannopyranosyloxy)-

3′,3′′′-(1,6-Hexanediyl)bis[6′-(α-D-mannopyranosyloxy)[1,1′-biphenyl]-3-acetic acid

TBC 1269

Bimosiamose