| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Quinagoguel is rapidly and extensively absorbed, with 95% of the oral dose being absorbed. However, due to first-pass metabolism, its absolute bioavailability is low (4%). Peak plasma concentration is reached in 30–60 minutes. At the recommended therapeutic dose, quinagoguel's prolactin-lowering effect occurs within 2 hours of administration, peaks within 4–6 hours, and lasts for at least 24 hours. Over 95% of the total dose is excreted as metabolites, with roughly equal amounts excreted in urine and feces. Renal excretion accounts for 50% of total excretion, with sulfate or glucuronide conjugates, N-deethyl, and N,N-dideethyl analogs detectable in urine. Free forms of sulfate or glucuronide conjugates, N-deethyl, and N,N-dideethyl analogs are excreted in feces, accounting for 40% of total drug excretion. The volume of distribution after a single oral dose is approximately 100 liters. It is expected that the active ingredient and its metabolites will be widely distributed in the extravascular space, with the main target organs being the liver, kidneys, salivary glands, and pituitary gland. Metabolism / Metabolites Quinagolide undergoes extensive first-pass metabolism, with sulfate and glucuronide conjugates being the major circulating metabolites. N-deethyl analogs are biologically active metabolites, while sulfate or glucuronide conjugates and N,N-dideethyl analogs are inactive. Known human metabolites of quinagolide include (2S,3S,4S,5R)-6-[[(3S,4aS,10aR)-3-(diethylsulfonamidoamino)-1-propyl-3,4,4a,5,10,10a-hexahydro-2H-benzo[g]quinolin-6-yl]oxy]-3,4,5-trihydroxyoxacyclohexane-2-carboxylic acid. Biological Half-Life The terminal half-life of the parent drug after a single dose is 11.5 hours, and the terminal half-life under steady state is 17 hours. |
|---|---|
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of use during lactation Quinagolite has not yet been approved for marketing by the U.S. Food and Drug Administration (FDA). It is a selective dopamine D2 receptor agonist that lowers serum prolactin levels. Because quinagolite inhibits lactation, it is generally not used in lactating women. There is currently no published information on the use of quinagolite in lactating women. ◉ Effects on breastfed infants As of the revised date, no relevant published information has been found. ◉ Effects on lactation and breast milk A small preliminary study compared the effects of quinagolite (CV 205-502) with bromocriptine starting treatment on the first day postpartum for 21 days in mothers who did not wish to breastfeed. Serum prolactin levels returned to normal more quickly in the bromocriptine group, while more women in the quinagolite group experienced breast symptoms. The effects of inhibiting lactation were similar in both groups. [1] Protein Binding According to reports, plasma protein binding is nonspecific, with a rate of approximately 90%. |
| References |
| Molecular Formula |
C20H33N3O3S
|
|---|---|
| Molecular Weight |
395.56
|
| Exact Mass |
395.224
|
| CAS # |
87056-78-8
|
| PubChem CID |
3086401
|
| Appearance |
Typically exists as solids at room temperature
|
| Density |
1.23g/cm3
|
| Boiling Point |
539.1ºC at 760mmHg
|
| Melting Point |
231-237
|
| Flash Point |
279.8ºC
|
| Index of Refraction |
1.598
|
| LogP |
3.546
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
27
|
| Complexity |
576
|
| Defined Atom Stereocenter Count |
3
|
| SMILES |
CCCN1C[C@H](C[C@@H]2CC3=C(C=CC=C3O)C[C@H]21)NS(=O)(=O)N(CC)CC
|
| InChi Key |
GDFGTRDCCWFXTG-ZIFCJYIRSA-N
|
| InChi Code |
InChI=1S/C20H33N3O3S/c1-4-10-22-14-17(21-27(25,26)23(5-2)6-3)11-16-12-18-15(13-19(16)22)8-7-9-20(18)24/h7-9,16-17,19,21,24H,4-6,10-14H2,1-3H3/t16-,17+,19-/m1/s1
|
| Chemical Name |
(3S,4aS,10aR)-3-(diethylsulfamoylamino)-6-hydroxy-1-propyl-3,4,4a,5,10,10a-hexahydro-2H-benzo[g]quinoline
|
| Synonyms |
Quinagolide; CV205-502
|
| 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 (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
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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 : PEG300 ：Tween 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). View More
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)] 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). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5281 mL | 12.6403 mL | 25.2806 mL | |
| 5 mM | 0.5056 mL | 2.5281 mL | 5.0561 mL | |
| 10 mM | 0.2528 mL | 1.2640 mL | 2.5281 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.
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.
Link: https://clinicaltrials.gov/ct2/show/NCT00329693
Conditions:Ovarian Hyperstimulation SyndromeLink: https://clinicaltrials.gov/ct2/show/NCT00665041
Conditions:Ovarian Hyperstimulation SyndromeProducts are for research use only; We do not sell to patients
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