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| Targets |
LHCGR (luteinizing hormone/chorionic gonadotropin receptor) and TSHR (thyroid-stimulating hormone receptor). Org-41841 is a partial agonist of both LHCGR and TSHR. LHCGR is a G protein-coupled receptor that mediates the effects of luteinizing hormone and chorionic gonadotropin, playing a critical role in reproductive function, including ovulation and testosterone production. TSHR is a G protein-coupled receptor that mediates the effects of thyroid-stimulating hormone, regulating thyroid hormone production and metabolism. By activating these receptors, Org-41841 can regulate hormone secretion and reproductive function. Org-41841 has EC50 values of 0.2 μM for LHCGR and 7.7 μM for TSHR. The compound can be used to study hyperthyroidism.
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| ln Vitro |
Org41841 is a partial agonist of the thyroid stimulating hormone receptor (TSHR) and luteinizing hormone/chorionic gonadotropin receptor (LHCGR), with EC50 values of 0.2 and 7.7 μM, respectively, according to functional testing. After treating L570F with Org41841, the EC50 increased to 800 nM. M9 reacts to Org41841 by increasing its EC50 to 2700 nM and significantly increasing its signaling efficacy, which reaches 99% of the maximum value recorded for activation of the thyroid-stimulating hormone receptor (TSHR) by thyroid-stimulating hormone (TSH) [1].
Org-41841 is a partial agonist of LHCGR and TSHR with EC50 values of 0.2 μM and 7.7 μM, respectively. The compound's activity has been characterized in receptor binding and functional assays measuring receptor-mediated signaling (e.g., cAMP accumulation). Org-41841 directly activates LHCGR and TSHR to regulate hormone secretion. The compound can be used to study hyperthyroidism. Org-41841's partial agonist activity distinguishes it from full agonists and may result in a different pharmacological profile. |
| ln Vivo |
Org-41841 has been studied in vivo for its effects on hormone secretion and thyroid function. As a partial agonist of LHCGR and TSHR, it can regulate hormone secretion and reproductive function. The compound can be used to study hyperthyroidism. Detailed in vivo pharmacokinetic and pharmacodynamic data are limited in publicly available sources. Org-41841 is for research use only and is not for human therapeutic use.
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| Enzyme Assay |
LHCGR and TSHR binding assays are performed using membranes prepared from cells expressing recombinant LHCGR or TSHR. Radioligand binding studies use [¹²⁵I]-hCG (LHCGR) or [¹²⁵I]-TSH (TSHR) as labeled ligands. Membrane preparations are incubated with varying concentrations of Org-41841 and a fixed concentration of radioligand in binding buffer for 60-120 minutes at room temperature. Non-specific binding is determined using excess unlabeled hCG or TSH. Bound radioactivity is measured by gamma counting after filtration. IC50 and Ki values are calculated by non-linear regression. Functional assays measure receptor-mediated cAMP accumulation in response to receptor activation.
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| Cell Assay |
Cellular LHCGR and TSHR activation is evaluated in cell lines expressing recombinant LHCGR or TSHR (e.g., HEK-293 cells). Cells are cultured in appropriate media at 37°C with 5% CO₂ and treated with Org-41841 at various concentrations. Functional assays measure receptor-mediated cAMP accumulation. The compound's agonist activity is assessed by its ability to stimulate cAMP production. Cell viability is assessed using MTT or LDH assays. Each experiment includes known LHCGR/TSHR agonists (e.g., hCG, TSH) as positive controls and vehicle controls.
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| Animal Protocol |
In vivo efficacy of Org-41841 is evaluated in animal models of hyperthyroidism and reproductive disorders. The compound is administered orally or intraperitoneally at doses determined by preclinical studies. Hormone levels (e.g., thyroid hormones, LH, FSH, testosterone) are measured in serum by ELISA or RIA. Thyroid and reproductive organ function are assessed by histopathology and biochemical assays. Sample sizes typically range from 6-10 animals per group.
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| ADME/Pharmacokinetics |
Molecular Weight: 402.53. Formula: C19H22N4O2S2. CAS No.: 301847-37-0. Chemical Name: 5-amino-N-tert-butyl-4-(3-methoxyphenyl)-2-(methylsulfanyl)thieno[2,3-d]pyrimidine-6-carboxamide. Synonyms: Org41841; Org-41841. Appearance: Solid. Purity: Typically >98%. Solubility: Soluble in DMSO. Storage: Powder at -20°C for up to 3 years; In solvent at -20°C for up to 6 months. Org-41841 is a partial agonist of LHCGR and TSHR with EC50s of 0.2 and 7.7 μM.
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| Toxicity/Toxicokinetics |
No comprehensive toxicology data are publicly available for Org-41841. The compound is intended for research use only and has not undergone full preclinical toxicology evaluation required for clinical development. As an LHCGR and TSHR agonist, potential toxicities may include hormonal imbalances and effects on reproductive and thyroid function. Standard toxicity studies would include acute toxicity assessment in rodents, repeated dose toxicity studies (14-day and 28-day), and genotoxicity screening (Ames test, micronucleus assay). The compound is for research use only and not for human therapeutic use.
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| References | |
| Additional Infomation |
5-Amino-N-tert-butyl-4-(3-methoxyphenyl)-2-(methylthio)-6-thieno[2,3-d]pyrimidine carboxamide is a pyrimidine compound and also a thienopyrimidine compound.
Org-41841 is also known as Org41841. Its chemical name is 5-amino-N-tert-butyl-4-(3-methoxyphenyl)-2-(methylsulfanyl)thieno[2,3-d]pyrimidine-6-carboxamide. Org-41841 is a partial agonist of both LHCGR and TSHR with EC50s of 0.2 and 7.7 μM, respectively. The compound directly activates the receptors to regulate hormone secretion and reproductive function. Org-41841 can be used to study hyperthyroidism. No clinical trials have been reported for this compound. Org-41841 is for research use only. |
| Molecular Formula |
C19H22N4O2S2
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| Molecular Weight |
402.533581256866
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| Exact Mass |
402.118
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| CAS # |
301847-37-0
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| PubChem CID |
9887381
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| Appearance |
White to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Index of Refraction |
1.670
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| LogP |
4.34
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
27
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| Complexity |
530
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
DVSFSADBOJYPGF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H22N4O2S2/c1-19(2,3)23-16(24)15-13(20)12-14(10-7-6-8-11(9-10)25-4)21-18(26-5)22-17(12)27-15/h6-9H,20H2,1-5H3,(H,23,24)
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| Chemical Name |
5-amino-N-tert-butyl-4-(3-methoxyphenyl)-2-methylsulfanylthieno[2,3-d]pyrimidine-6-carboxamide
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~248.43 mM)
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| 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 | 2.4843 mL | 12.4214 mL | 24.8429 mL | |
| 5 mM | 0.4969 mL | 2.4843 mL | 4.9686 mL | |
| 10 mM | 0.2484 mL | 1.2421 mL | 2.4843 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.
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