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Goralatide acetate

Cat No.:V48924 Purity: ≥98%
Goralatide acetate, the acetate salt of Goralatide, isa novel , tetrapeptide-based inhibitor of cell cycle progression with anticancer activity.
Goralatide acetate
Goralatide acetate Chemical Structure Product category: Peptides
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
15mg
25mg
50mg
100mg
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Other Forms of Goralatide acetate:

  • Goralatide TFA
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description
Goralatide acetate, the acetate salt of Goralatide, is a novel , tetrapeptide-based inhibitor of cell cycle progression with anticancer activity.
Goralatide acetate is the acetate salt of Goralatide (Ac-SDKP), a natural tetrapeptide that functions as a physiological regulator of hematopoiesis. The peptide sequence is N-acetyl-serine-aspartate-lysine-proline (Ac-SDKP). Goralatide is a physiological substrate of angiotensin I-converting enzyme (ACE). The compound has a molecular weight of 547.56 g/mol. Goralatide is a synthetic tetrapeptide derived from thymosin beta-4 and is classified as a peptide hormone and hematopoietic regulator. It is used in research on hematopoiesis and stem cell biology.
Biological Activity I Assay Protocols (From Reference)
Targets
Goralatide targets primitive hematopoietic stem cells and progenitors. It functions as a physiological regulator of hematopoiesis by inhibiting the entry of hematopoietic stem cells into the S-phase of the cell cycle. Goralatide inhibits primitive hematopoietic cell proliferation. The compound is a physiological substrate of ACE, which cleaves and inactivates the tetrapeptide. By maintaining hematopoietic stem cells in a quiescent state, Goralatide plays a role in the regulation of hematopoietic homeostasis and may protect stem cells from damage during chemotherapy.
ln Vitro
In vitro, Goralatide inhibits the proliferation of primitive hematopoietic cells. The compound acts as a physiological regulator of hematopoiesis, maintaining hematopoietic stem cells in a quiescent state by preventing their entry into the S-phase of the cell cycle. Studies using hematopoietic stem cell cultures demonstrate that Goralatide reduces the proliferation of primitive progenitor cells while sparing more differentiated cells. The compound is also a substrate for ACE, which cleaves the tetrapeptide and regulates its activity. Goralatide is used as a research tool to study hematopoietic stem cell biology and regulation.
ln Vivo
In vivo, Goralatide acts as a physiological regulator of hematopoiesis. Studies in animal models demonstrate that Goralatide inhibits the proliferation of primitive hematopoietic cells and maintains stem cell quiescence. The compound has been investigated for its potential to protect hematopoietic stem cells from the cytotoxic effects of chemotherapy by keeping them in a quiescent state, thereby reducing chemotherapy-induced myelosuppression. Goralatide is also a substrate for ACE, which regulates its activity in vivo. Further studies are needed to fully characterize its in vivo efficacy.
Enzyme Assay
In vitro assays for Goralatide typically involve hematopoietic stem and progenitor cell cultures. The standard protocol includes isolating murine or human hematopoietic stem cells (Lin⁻Sca-1⁺c-Kit⁺ cells or CD34⁺ cells) and culturing them with Goralatide at concentrations ranging from 0.1-100 µM. Cell proliferation is assessed by thymidine incorporation, CFU (colony-forming unit) assays, or flow cytometry analysis of cell cycle status (Ki67 or BrdU staining). The ability of Goralatide to maintain stem cell quiescence is evaluated by measuring the proportion of cells in G₀ phase.
Cell Assay
Cell-based assays for Goralatide are conducted in hematopoietic stem and progenitor cell cultures. Cells are isolated from bone marrow or umbilical cord blood and cultured with Goralatide at varying concentrations (0.1-100 µM) for 24-72 hours. Cell cycle analysis is performed by flow cytometry using Ki67 and Hoechst or DAPI staining to distinguish G₀, G₁, and S/G₂/M phases. Proliferation is assessed by CFU assays in semisolid media (methylcellulose) with cytokines. Apoptosis is evaluated by Annexin V staining. The effects of Goralatide on stem cell differentiation are assessed by flow cytometry for lineage markers.
Animal Protocol
In vivo animal experiments for Goralatide typically use mouse models. Animals are administered Goralatide via subcutaneous or intraperitoneal injection at doses of 0.1-10 mg/kg. Bone marrow and peripheral blood are collected at various time points for analysis of hematopoietic stem and progenitor cell numbers, cell cycle status, and colony-forming ability. The compound's effects on chemotherapy-induced myelosuppression are evaluated by administering Goralatide before or after chemotherapy and measuring recovery of blood cell counts. The in vivo activity of Goralatide is also regulated by ACE-mediated cleavage.
ADME/Pharmacokinetics
Pharmacokinetic data for Goralatide are limited. As a tetrapeptide, the compound is expected to have rapid clearance due to proteolytic degradation, particularly by ACE which cleaves Ac-SDKP. The compound has a short half-life in circulation. Goralatide acetate is a peptide that may require formulation for in vivo administration. Storage: typically at -20°C for long-term storage. Purity is typically >98%. The compound is soluble in aqueous solutions and DMSO. Further PK studies would be required for comprehensive characterization.
Toxicity/Toxicokinetics
Toxicity data for Goralatide acetate are limited. The compound is a natural tetrapeptide and physiological regulator of hematopoiesis. It is supplied for research use only and is not intended for human administration. As a peptide, it is expected to have low toxicity. Standard laboratory safety precautions should be followed. No specific toxicological studies have been published. The compound should be handled with care and stored appropriately.
References

Additional Infomation
Goralatide acetate (Ac-SDKP) is a research compound supplied for laboratory use only. It is not an approved drug and has no clinical trial or marketing authorization status. The compound is a natural tetrapeptide that functions as a physiological regulator of hematopoiesis. It inhibits primitive hematopoietic cell proliferation and is a substrate for ACE. Purity is typically >98%. The compound appears as a white to off-white solid and should be stored appropriately.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C22H37N5O11
Molecular Weight
547.56
Related CAS #
Goralatide TFA;1796568-94-9
Appearance
White to off-white solid powder
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
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)
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.57 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 (4.57 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 25.0 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.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (4.57 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.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.8263 mL 9.1314 mL 18.2628 mL
5 mM 0.3653 mL 1.8263 mL 3.6526 mL
10 mM 0.1826 mL 0.9131 mL 1.8263 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.

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:
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  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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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.

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