YM-254890

Alias: YM254890; YM 254890; YM-254890

Cat No.:V4938 Purity: ≥98%

COA Product Data Instructions for use SDS

YM-254890 (YM254890),a cyclic depsipeptide discovered from Chromobacterium sp.

YM-254890 Chemical Structure CAS No.: 568580-02-9
Product category: New7

This product is for research use only, not for human use. We do not sell to patients.

Size	Price	Stock	Qty
1mg
Other Sizes

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1-708-310-1919 sales@invivochem.com

Other Forms of YM-254890:

WU-07047

Official Supplier of:

Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

Science Adv 2022: 8, eabm9427.

Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

Science Trans Med 2023,15(701):eadd7872.

STTT 2023,8(1):91.

Cell Reports 2023,42(4):112313

Science Trans Med 2023, 15: eadd7872.

Cancer Cell 2021,39(4):529-547.e7.

Cancer Discov 2022,12(4):1106-1127.

Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Biological Data

Product Description

YM-254890 (YM254890), a cyclic depsipeptide discovered from Chromobacterium sp. QS3666 culture broth, is a novel, potent and specific Gαq/11 inhibitor with anti-platelet activity. It can inhibit adp-induced platelet aggregation and blocking gαq/11-coupled adp receptor p2y1-mediated ca2+ mobilization. YM-254890 concentration dependently inhibited ADP-induced intracellular Ca2+ elevation, with an IC50 value of 0.92±0.28 μm. YM-254890 had no effect on the binding of fibrinogen to purified GPIIb/IIIa, but strongly inhibited binding to TRAP-stimulated washed platelets.

Biological Activity I Assay Protocols (From Reference)

ln Vitro	With IC50 values of 0.37, 0.39, and 0.51 μM, YM-254890 suppresses platelet aggregation in human platelet-rich plasma that is triggered by ADP (2, 5, and 20 μM). Platelet aggregation is mediated by ADP via the G protein-coupled receptors P2Y1 and P2Y12. C6-15 cells that transiently expressed human P2Y1 or P2Y12 receptors were used to investigate the effects of YM-254890 on the P2Y1 and P2Y12 signaling pathways. When 2MeSADP is used to stimulate P2Y1-C6-15 cells, there is a greater intracellular calcium mobilization. With an IC50 value of 0.031 μM, YM-254890 suppresses the rise in [Ca2+]i in this experiment. On the other hand, in P2Y12-C6-15 cells, YM-254890 at 40 μM had no effect on the 2MeSADP-induced suppression of forskolin-stimulated adenylyl cyclase activity [1].
References	[1]. Taniguchi M, et al. YM-254890, a novel platelet aggregation inhibitor produced by Chromobacterium sp. QS3666. J Antibiot (Tokyo). 2003 Apr;56(4):358-63. [2]. Zhang H, et al. Structure-activity relationship and conformational studies of the natural product cyclic depsipeptides YM-254890 and FR900359. Eur J Med Chem. 2018 Aug 5;156:847-860.

ln Vitro

With IC50 values of 0.37, 0.39, and 0.51 μM, YM-254890 suppresses platelet aggregation in human platelet-rich plasma that is triggered by ADP (2, 5, and 20 μM). Platelet aggregation is mediated by ADP via the G protein-coupled receptors P2Y1 and P2Y12. C6-15 cells that transiently expressed human P2Y1 or P2Y12 receptors were used to investigate the effects of YM-254890 on the P2Y1 and P2Y12 signaling pathways. When 2MeSADP is used to stimulate P2Y1-C6-15 cells, there is a greater intracellular calcium mobilization. With an IC50 value of 0.031 μM, YM-254890 suppresses the rise in [Ca2+]i in this experiment. On the other hand, in P2Y12-C6-15 cells, YM-254890 at 40 μM had no effect on the 2MeSADP-induced suppression of forskolin-stimulated adenylyl cyclase activity [1].

References

[1]. Taniguchi M, et al. YM-254890, a novel platelet aggregation inhibitor produced by Chromobacterium sp. QS3666. J Antibiot (Tokyo). 2003 Apr;56(4):358-63.
[2]. Zhang H, et al. Structure-activity relationship and conformational studies of the natural product cyclic depsipeptides YM-254890 and FR900359. Eur J Med Chem. 2018 Aug 5;156:847-860.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula	C46H69N7O15
Molecular Weight	960.077973127365
CAS #	568580-02-9
Related CAS #	568580-02-9 (YM-254890); 1702378-78-6 ( WU-07047, a simplified analog of the selective Gαq/11 inhibitor YM-25489)
SMILES	CC(C)[C@@H](O)[C@H](NC(C)=O)C(O[C@@H]([C@H](NC([C@H](C)N(C)C([C@H](C)NC(C(N(C)C([C@@H](CC1=CC=CC=C1)O2)=O)=C)=O)=O)=O)C(N(C)[C@@H]([C@H](OC)C)C(O[C@H](C)[C@H](NC(C)=O)C2=O)=O)=O)C(C)C)=O
InChi Key	QVYLWCAYZGFGNF-WBWCVGBTSA-N
InChi Code	InChI=1S/C46H69N7O15/c1-22(2)37(56)34(49-30(11)55)45(63)68-38(23(3)4)35-43(61)53(14)36(28(9)65-15)46(64)66-27(8)33(48-29(10)54)44(62)67-32(21-31-19-17-16-18-20-31)42(60)52(13)25(6)39(57)47-24(5)41(59)51(12)26(7)40(58)50-35/h16-20,22-24,26-28,32-38,56H,6,21H2,1-5,7-15H3,(H,47,57)(H,48,54)(H,49,55)(H,50,58)/t24-,26-,27+,28+,32+,33-,34-,35-,36-,37+,38+/m0/s1
Chemical Name	(R)-1-((3S,6S,9S,12S,18R,21S,22R)-21-Acetamido-18-benzyl-3-((R)-1-methoxyethyl)-4,9,10,12,16,22-hexamethyl-15-methylene-2,5,8,11,14,17,20-heptaoxo-1,19-dioxa-4,7,10,13,16-pentaazacyclodocosan-6-yl)-2-methylpropyl (2S,3R)-2-acetamido-3-hydroxy-4-methylpentanoate
Synonyms	YM254890; YM 254890; YM-254890
Storage	Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)	DMSO : ~50 mg/mL (~52.08 mM)
Solubility (In Vivo)	Solubility in Formulation 1: ≥ 1.25 mg/mL (1.30 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (1.30 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More Solubility in Formulation 3: ≥ 1.25 mg/mL (1.30 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.)

Solubility (In Vitro)

DMSO : ~50 mg/mL (~52.08 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 1.25 mg/mL (1.30 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 1.25 mg/mL (1.30 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

View More

Solubility in Formulation 3: ≥ 1.25 mg/mL (1.30 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

(Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	1.0416 mL	5.2079 mL	10.4158 mL
	5 mM	0.2083 mL	1.0416 mL	2.0832 mL
	10 mM	0.1042 mL	0.5208 mL	1.0416 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

Concentration

Volume

Molecular Weight*

Calculate Reset

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

Number of animals

Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Biological Data

Effects of YM-254890 (a) and MRS2179 (b) on ADP-induced human platelet intracellular Ca2+elevation.Br J Pharmacol. 2006 May; 148(1): 61–69.
Effects of YM-254890 and MRS2179 on P-selectin expression and fibrinogen binding.Br J Pharmacol. 2006 May; 148(1): 61–69.
Effect of YM-254890 on human platelet shape change after the addition of various agonists.
Effect of YM-254890 on SIPA in human PRP.Br J Pharmacol. 2006 May; 148(1): 61–69.