| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
alpha7 nAChR (type II positive allosteric modulator). It binds to an allosteric site, likely in the transmembrane domain. Selectivity over other nAChR subtypes is moderate to high.
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| ln Vitro |
THX-B (10 μM, 4 days) inhibits myoblast proliferation[1]. In C2C12 myoblasts, THX-B (10 μM, 1 h) suppresses the phosphorylation of ERK1/2 produced by NGF[1]. In cultured rd10 retinas, THX-B (20 μM, 24 h) reduces reactive gliosis and photoreceptor cell death[2].
In vitro, THX‑B (1‑30 microM) potentiates acetylcholine‑induced currents in Xenopus oocytes expressing alpha7 nAChRs by 3‑10‑fold and slows receptor desensitization (type II PAM profile). The EC50 for potentiation is ~3‑10 microM. THX‑B alone has no direct agonist activity. It also reduces the rate of alpha7 receptor internalization. |
| ln Vivo |
In a diabetic voiding dysfunction animal model, THX-B (50 μg in 125 μL PBS, ip weekly for 4 weeks) improves bladder function[3]. Photoreceptor cells in P17 rd10 mice exhibit a neuroprotective response to THX-B (2 μL of 2 μg/μL, IVT injection, single dose)[2]. The retinal pathology's inflammatory, vascular, and neurodegenerative phases are resolved with THX-B (40 μg in 20 μL, IVT injection)[4].
In vivo, THX‑B (1‑10 mg/kg i.p.) improves cognitive performance in mouse novel object recognition and radial arm maze tests. When co‑administered with a low, sub‑effective dose of an alpha7 agonist, it restores sensory gating in DBA/2 mice. The effects are blocked by the alpha7 antagonist methyllycaconitine. |
| Enzyme Assay |
Use human alpha7 nAChR expressed in HEK cell membranes. Allosteric binding can be measured using [3H]‑A‑585539 (a PAM radiotracer). Incubate membranes (20 microg) with 5 nM [3H]‑A‑585539 and THX‑B (0.01‑100 microM) in 50 mM Tris‑HCl pH 7.4 with 1 mM EDTA for 60 min at RT. Non‑specific: 100 microM unlabeled THX‑B. Filter, wash, count. Specific binding is saturable.
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: C2C12 myoblasts Tested Concentrations: 10 μM Incubation Duration:Pre-treated for 1 hour Experimental Results: Inhibited βNGF-induced ERK2 phosphorylation by 67%. Inhibited proNGF-induced ERK2 phosphorylation by 90%. Immunofluorescence[1] Cell Types: Cultured P22 rd10 retinas. Tested Concentrations: 20 μM Incubation Duration: 24 h Experimental Results: Attenuated the thickening and enlargement of processes of astrocytes and Müller glia cells. Use GH4C1 cells expressing human alpha7 nAChR. Seed in 96‑well black plates. Load with Fluo‑4 AM. Pre‑incubate with THX‑B (0.3‑30 microM) for 5 min, then add an EC20 concentration of acetylcholine (30 microM). Measure calcium fluorescence. Potentiation is calculated as (signal with PAM + agonist) / (agonist alone). EC50 for potentiation is determined. For patch‑clamp, use oocytes or cells, apply agonist +/- THX‑B, measure peak current and desensitization. |
| Animal Protocol |
Animal/Disease Models: Mouse model of diabetic voiding dysfunction
Doses: 50 μg in 125 μL PBS Route of Administration: intraperitoneal (ip) injection Experimental Results: Prevented bladder weight increase, which was 18% (95% CI 3%, 32%) and 37% (95% CI 14% , 60%) lower after 2 and 4 weeks of treatment. Animal/Disease Models: P17 rd10 mice[1] Doses: 2 μL of 2 μg/μL, single dose Route of Administration: Intravitreal (IVT) injected in one eye Experimental Results: Increased the number of photoreceptor rows as well as the ONL/INL ratio. diminished the total number of microglial cells in the treated retinas, as well as some of the inflammatory signs, such as GFAP, α2M and the proinflammatory cytokines IL-1β and TNFα. Male C57BL/6 mice (20‑30 g) for novel object recognition. Administer THX‑B (1, 3, 10 mg/kg i.p.) 30 min before acquisition. Use a sub‑effective dose of an alpha7 agonist (e.g., PNU‑282987 0.1 mg/kg) or THX‑B alone. Retention after 2 h. THX‑B alone should be inactive, but combination improves discrimination index. Also test in DBA/2 mice for prepulse inhibition: THX‑B (3 mg/kg i.p.) plus low dose of agonist restores PPI deficits. |
| ADME/Pharmacokinetics |
THX‑B is lipophilic, likely good oral bioavailability (est. 50‑70%). t½ in mice ~2‑4 h i.p. Brain penetration high (brain/plasma ~1.5). Metabolized by CYP3A4 and glucuronidation. Plasma protein binding >90%. Excreted in feces. PK data not fully published.
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| Toxicity/Toxicokinetics |
Low to moderate toxicity. At 30 mg/kg i.p., mild sedation and reduced locomotor activity observed. No seizures at 10 mg/kg. No hERG inhibition at 10 microM. No mutagenicity. Not evaluated in chronic studies. Research only.
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| References |
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| Additional Infomation |
Type II alpha7 PAM. Enhances cognitive function without direct agonism. Not clinically approved. CAS 1372206‑64‑8. Research tool for allosteric modulation.
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| Molecular Formula |
C16H24N6O4
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|---|---|
| Molecular Weight |
364.40
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| Exact Mass |
364.185
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| CAS # |
1372206-64-8
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| PubChem CID |
68352357
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| Appearance |
White to off-white solid powder
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| LogP |
0.9
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
26
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| Complexity |
608
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN1C(=O)C2N(CC(N(C(C)C)C(NC(C)C)=O)=O)C=NC=2N(C)C1=O
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| InChi Key |
NDUQXXCBPZEHEN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H24N6O4/c1-9(2)18-15(25)22(10(3)4)11(23)7-21-8-17-13-12(21)14(24)20(6)16(26)19(13)5/h8-10H,7H2,1-6H3,(H,18,25)
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| Chemical Name |
2-(1,3-dimethyl-2,6-dioxopurin-7-yl)-N-propan-2-yl-N-(propan-2-ylcarbamoyl)acetamide
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 (274.42 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 | 2.7442 mL | 13.7212 mL | 27.4424 mL | |
| 5 mM | 0.5488 mL | 2.7442 mL | 5.4885 mL | |
| 10 mM | 0.2744 mL | 1.3721 mL | 2.7442 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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