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Deslorelin Acetate

Cat No.:V37127 Purity: ≥98%
Deslorelin Acetate is a novel and potent gonadotropin releasing hormone super-agonist (GnRH agonist)
Deslorelin Acetate
Deslorelin Acetate Chemical Structure CAS No.: 82318-06-7
Product category: Peptides
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
100mg
500mg
1g
Other Sizes

Other Forms of Deslorelin Acetate:

  • Deslorelin
Official Supplier of:
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Purity & Quality Control Documentation

Purity: =99.53%

Product Description
Deslorelin Acetate is a novel and potent gonadotropin releasing hormone super-agonist (GnRH agonist)
Deslorelin Acetate is a synthetic nonapeptide analogue of gonadotropin-releasing hormone (GnRH). It is a potent GnRH super-agonist (also known as an LHRH agonist). It features D-Trp6 and Pro-NHEt9 substitutions that confer enhanced receptor binding affinity and resistance to enzymatic degradation.
Biological Activity I Assay Protocols (From Reference)
Targets
Deslorelin Acetate targets the gonadotropin-releasing hormone receptor (GnRHR). As a GnRH superagonist, it binds to and activates the GnRH receptor, leading to an initial stimulation of gonadotropin release. With continued administration, it causes downregulation of the receptor, resulting in suppression of sex hormone production.
ln Vitro
In vitro, Deslorelin Acetate is a potent GnRH agonist. It is used in cell-based assays to study GnRH receptor signaling and the regulation of gonadotropin secretion. Its activity is related to its ability to bind to and activate the GnRH receptor.
ln Vivo
In vivo, Deslorelin Acetate is used in veterinary medicine to control estrus and fertility in animals, including dogs, cats, and horses. It is also used in the treatment of precocious puberty. Research on this compound explores its applications in assisted reproductive technologies and wildlife contraception.
Enzyme Assay
In vitro receptor binding assays for Deslorelin Acetate typically involve measuring its affinity for the GnRH receptor. The compound is incubated with cells expressing the receptor, and binding is quantified. Functional assays, such as measuring gonadotropin release upon receptor activation, are also used to confirm its agonistic activity.
Cell Assay
Cell culture protocols for Deslorelin Acetate involve treating pituitary cells or cells expressing the GnRH receptor with the compound at varying concentrations. The effects on gonadotropin secretion and cell signaling are then assessed. The peptide is dissolved in a suitable solvent and added to the culture medium.
Animal Protocol
In vivo animal study protocols for Deslorelin Acetate involve its administration to animals to study its effects on reproduction. It is commonly used in veterinary medicine for estrus control and ovulation induction. In research, it is used to study the hypothalamic-pituitary-gonadal axis and reproductive function.
ADME/Pharmacokinetics
Deslorelin Acetate has a molecular weight of 1342.53 g/mol and a formula of C66H87N17O14. It has a CAS number of 82318-06-7. It is typically stored as a powder at -20°C. It is soluble in aqueous solutions and is available with high purity.
Toxicity/Toxicokinetics
Toxicological data for Deslorelin Acetate is not extensively reported in the provided sources. As a veterinary therapeutic agent, its safety profile has been established in animals. Standard safety precautions should be observed in research settings.
Additional Infomation
Deslorelin acetate is a synthetic nonapeptide natural gonadotropin-releasing hormone (GnRH) analog with potential antitumor activity. Deslorelin binds to and activates pituitary GnRH receptors. In males, sustained, long-term use of goserelin leads to pituitary GnRH receptor desensitization and inhibits the secretion of follicle-stimulating hormone (FSH) and luteinizing hormone (LH), thereby significantly reducing testosterone levels; in females, long-term use leads to decreased estradiol levels. (NCI04)
See also: Deslorelin (containing the active ingredient); Deslorelin; Deslorelin acetate (ingredient).
Pharmaceutical Indications
For inducing temporary infertility in healthy, unsterilized, sexually mature male dogs and ferrets.
Deslorelin Acetate has a CAS number of 82318-06-7. It is a synthetic GnRH superagonist used in veterinary medicine for reproductive management. It has potential antitumor activity and is also used in research on assisted reproductive technologies and wildlife conservation.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C64H83N17O12.C2H4O2
Molecular Weight
1342.50248
Exact Mass
1341.661
CAS #
82318-06-7
Related CAS #
57773-65-6;82318-06-7 (acetate);1642579-30-3;
PubChem CID
25077533
Appearance
Typically exists as solid at room temperature
Hydrogen Bond Donor Count
17
Hydrogen Bond Acceptor Count
16
Rotatable Bond Count
32
Heavy Atom Count
97
Complexity
2640
Defined Atom Stereocenter Count
9
SMILES
CCNC([C@H]1CCCN1C([C@@H](NC([C@@H](NC([C@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H]2CCC(N2)=O)=O)CC3=CN=CN3)=O)CC4=CNC5=CC=CC=C45)=O)CO)=O)CC6=CC=C(O)C=C6)=O)CC7=CNC8=CC=CC=C78)=O)CC(C)C)=O)CCCNC(N)=N)=O)=O.CC(O)=O
InChi Key
LYCYLGFSIXIXAB-NUZRHMIVSA-N
InChi Code
InChI=1S/C64H83N17O12.C2H4O2/c1-4-68-62(92)53-16-10-24-81(53)63(93)46(15-9-23-69-64(65)66)74-56(86)47(25-35(2)3)75-58(88)49(27-37-30-70-43-13-7-5-11-41(37)43)77-57(87)48(26-36-17-19-40(83)20-18-36)76-61(91)52(33-82)80-59(89)50(28-38-31-71-44-14-8-6-12-42(38)44)78-60(90)51(29-39-32-67-34-72-39)79-55(85)45-21-22-54(84)73-45;1-2(3)4/h5-8,11-14,17-20,30-32,34-35,45-53,70-71,82-83H,4,9-10,15-16,21-29,33H2,1-3H3,(H,67,72)(H,68,92)(H,73,84)(H,74,86)(H,75,88)(H,76,91)(H,77,87)(H,78,90)(H,79,85)(H,80,89)(H4,65,66,69);1H3,(H,3,4)/t45-,46-,47-,48-,49+,50-,51-,52-,53-;/m0./s1
Chemical Name
acetic acid;(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-[(2S)-2-(ethylcarbamoyl)pyrrolidin-1-yl]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide
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

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)
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

Injection Formulations
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO 400 μLPEG300 50 μL Tween 80 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).
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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO 900 μL (20% SBE-β-CD in saline)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL Saline)


Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).
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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 0.7449 mL 3.7244 mL 7.4488 mL
5 mM 0.1490 mL 0.7449 mL 1.4898 mL
10 mM 0.0745 mL 0.3724 mL 0.7449 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

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
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.

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
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
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.
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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)
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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