Thiazovivin

Alias: Thiazovivin; TZV
Cat No.:V1343 Purity: ≥98%
Thiazovivin (TZV) is a novel, selective, and cell-permeable small molecule ROCK (Rho-associated kinase) inhibitor with an IC50 of 0.5 μM in a cell-free assay.
Thiazovivin Chemical Structure CAS No.: 1226056-71-8
Product category: ROCK
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Thiazovivin (TZV) is a novel, selective, and cell-permeable small molecule ROCK (Rho-associated kinase) inhibitor with an IC50 of 0.5 μM in a cell-free assay. It can protect human embryonic stem cells (hESC). Thiazovivin promotes hESC survival after single-cell dissociation and improves stemness maintenance of embryo-derived stem-like cells under chemically defined culture conditions in cattle. Thiazovivin directly targets ROCK and increases expression of pluripotency factors. The process using thiazovivin could be easier, faster and more cost effective than transgene integration into somatic cells.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
One ROCK inhibitor is thiazovivin. Thiazovivin (2 μM) preserves human embryonic stem cells (hESC) via blocking ROCK activity. After separation, thiazovivin dramatically prolongs hESCs' lifespan while preserving their pluripotency. Thiazovivin improves integrin signaling mediated by cell-ECM adhesion. Additionally, thiazovivin stabilizes E-cadherin upon cell dissociation to prevent hESCs from dying in the absence of extracellular matrix [1]. Thiazovivin promotes primary colony development and cell attachment of bovine embryonic-derived stem cell-like cells (eSLC) on feeder layers. Thiazovivin promotes the growth of eSLC cultures during passage and augments putative colony growth. Moreover, in bovine eSLC, thiazovivin increases the expression of genes unique to the ectodermal lineage [2].
ln Vivo

Animal Protocol


References
[1]. Xu Y, et al. Revealing a core signaling regulatory mechanism for pluripotent stem cell survival and self-renewal by small molecules. Proc Natl Acad Sci U S A. 2010 May 4;107(18):8129-34.
[2]. Park S, et al. Thiazovivin, a Rho kinase inhibitor, improves stemness maintenance of embryo-derived stem-like cells under chemically defined culture conditions in cattle. Anim Reprod Sci. 2015 Oct;161:47-57
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C15H13N5OS
Molecular Weight
311.36
CAS #
1226056-71-8
Related CAS #
1226056-71-8
SMILES
O=C(C1=CSC(NC2=NC=NC=C2)=N1)NCC3=CC=CC=C3
Chemical Name
N-(phenylmethyl)-2-(4-pyrimidinylamino)-4-thiazolecarboxamide
Synonyms
Thiazovivin; TZV
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: 15 mg/mL (48.2 mM)
Water: 14 mg/mL (43.71 mM)
Ethanol:<1 mg/mL(slightly soluble or insoluble)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.03 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 25.0 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: ≥ 2.5 mg/mL (8.03 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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Solubility in Formulation 3: 30% PEG400+0.5% Tween80+5% propylene glycol:30 mg/mL


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.2117 mL 16.0586 mL 32.1172 mL
5 mM 0.6423 mL 3.2117 mL 6.4234 mL
10 mM 0.3212 mL 1.6059 mL 3.2117 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

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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?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

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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:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

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
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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.)
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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.

(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
  • Thiazovivin


    Novel synthetic small molecules dramatically increase hESC survival after single cell dissociation by enhancing cell-ECM mediated integrin activity.2010 May 4;107(18):8129-34.

  • Thiazovivin


    Tzv stabilizes E-cadherin after cell dissociation to protect hESCs from death under ECM-free conditions.2010 May 4;107(18):8129-34.

  • Thiazovivin


    Tzv is a novel ROCK inhibitor and Rho-ROCK axis regulates cell-ECM and cell-cell adhesion.2010 May 4;107(18):8129-34.

  • Thiazovivin


    Cell-cell interaction regulates cell-ECM interaction and contributes to survival and self-renewal of hESCs.2010 May 4;107(18):8129-34.

  • Thiazovivin


    hESCs maintained in mESCs culture condition have better survival and are dependent on different cell adhesion signaling for survival and self-renewal.2010 May 4;107(18):8129-34.

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