| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vivo |
L-368,899 (0.1, 0.3, 1 mg/kg; intravenous injection; single dosage) revealed dose-related antagonism to OT-stimulated uterine contractions with an in vivo AD50 value of 0.35 mg/kg [1]. L-368,899 (3, 10, 30 mg/kg; id; single dosage) suppresses the contractile impact of OT (AD50= 7 mg/kg) and has a long duration of action in vivo (>4 hours) (AD50: L-368,899 has to be OT reaction reduced by 50%) [1]. L-368,899 (10 mg/kg, oral; single dosage) demonstrates a bioavailability (AUC 0-6 hours) of 35% [1]. L-368,899 (0.54, 1.8, 5.4 mg/kg; IV; single dose) decreases oxytocin-induced and endogenous increases in plasma PGFM concentrations [2].
|
|---|---|
| Animal Protocol |
Animal/Disease Models: Adult female SD (SD (Sprague-Dawley)) rat (250-350 g) [1].
Doses: 0.1, 0.3, 1 mg/kg Route of Administration: intravenous (iv) (iv)injection; single. Experimental Results: Inhibition of OT-stimulated uterine contractions, AD50 value was 0.35 mg/kg. Animal/Disease Models: Adult female SD (SD (Sprague-Dawley)) rat (250-350 g) [1]. Doses: 3, 10, 30 mg/kg Route of Administration: Intraduodenal; single. Experimental Results: It has an antagonistic effect on OT-stimulated uterine contraction, with an AD50 of 7 mg/kg and a duration of more than 4 hrs (hrs (hours)). Animal/Disease Models: Adult female SD (SD (Sprague-Dawley)) rat (250-350 g) [1]. Doses: 10 mg/kg Route of Administration: po (po (oral gavage)) single dose. Experimental Results: demonstrated oral activity with bioavailability (AUC 0-6 hrs (hrs (hours))) of 35%. Animal/Disease Models: Mature Dorset cross ewes (53-57 kg; ovariectomy) [2]. Doses: 0.54, 1.8, 5.4 mg/kg (3, 10 and 30 µg/kg/min for 3 hrs (hrs (hours)); dissolved in 0.9% saline). Route of Administration: intravenous (iv) (iv)infusion; single. Experimental Results: The resulting increase in PGFM plasma concentration was Dramatically diminished in frequency (from 2.2 to 1.0 |
| References |
|
| Molecular Formula |
C26H42N4O5S2
|
|---|---|
| Molecular Weight |
554.7655
|
| Exact Mass |
590.236
|
| CAS # |
148927-60-0
|
| Related CAS # |
L-368,899 hydrochloride;160312-62-9
|
| PubChem CID |
9872389
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.31g/cm3
|
| Index of Refraction |
1.61
|
| LogP |
5.577
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
9
|
| Heavy Atom Count |
37
|
| Complexity |
1040
|
| Defined Atom Stereocenter Count |
4
|
| SMILES |
S(C([H])([H])[C@]12C([H])([H])C([H])([H])[C@]([H])(C([H])([H])[C@]1([H])N([H])C([C@]([H])(C([H])([H])C([H])([H])S(C([H])([H])[H])(=O)=O)N([H])[H])=O)C2(C([H])([H])[H])C([H])([H])[H])(N1C([H])([H])C([H])([H])N(C2=C([H])C([H])=C([H])C([H])=C2C([H])([H])[H])C([H])([H])C1([H])[H])(=O)=O
|
| InChi Key |
MWIASLNTAGRGGA-ZJPWWDJASA-N
|
| InChi Code |
InChI=1S/C26H42N4O5S2/c1-19-7-5-6-8-22(19)29-12-14-30(15-13-29)37(34,35)18-26-11-9-20(25(26,2)3)17-23(26)28-24(31)21(27)10-16-36(4,32)33/h5-8,20-21,23H,9-18,27H2,1-4H3,(H,28,31)/t20-,21+,23+,26-/m1/s1
|
| Chemical Name |
(2S)-2-amino-N-[(1S,2S,4R)-7,7-dimethyl-1-[[4-(2-methylphenyl)piperazin-1-yl]sulfonylmethyl]-2-bicyclo[2.2.1]heptanyl]-4-methylsulfonylbutanamide
|
| 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 | 1.8025 mL | 9.0127 mL | 18.0255 mL | |
| 5 mM | 0.3605 mL | 1.8025 mL | 3.6051 mL | |
| 10 mM | 0.1803 mL | 0.9013 mL | 1.8025 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
