XAP044 |
رقم الكتالوجGC18120
One-Click Copy Product Info
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XAP044 هو مضاد قوي وانتقائي لـ mGlu7
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 196928-50-4
Sample solution is provided at 25 µL, 10mM.
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XAP044 is a potent mGlu7 selective antagonist, with an IC50 value of 5.5μM[1]. XAP044 blocks mGlu7 signaling via a binding pocket localized in mGlu7's extracellular Venus flytrap domain, a region generally known for orthosteric agonist binding[2]. XAP044 has been widely used as a model compound for the development of a series of related derivatives to inhibit mGlu7 activity[3].
In vivo, a single subcutaneous injection of XAP044(30mg/kg) within 2 hours reversed mechanical hyperalgesia and ameliorated anxieties and depression-like behaviors in a mouse model of neuropathic pain[4]. A single intraperitoneal injection of XAP044 at a dose of 60mg/kg for 30 minutes alleviated physiological and congenital anxist-and depression-like behaviors in mice, and reduced freezing behavior during the acquisition phase of fear conditioning[5]. Intracerebroventricular infusion of 100µM XAP044 at a rate of 0.11µl/h via a micro-osmotic pump for 20 days improved hypothalamic-pituitary-adrenal axis dysfunction, thymic atrophy, and chronic subordinate colony housing (CSC)-induced increases in congenital anxiety in male C57BL/6 mice[6].
References:
[1] Fisher N M, Seto M, Lindsley C W, et al. Metabotropic glutamate receptor 7: a new therapeutic target in neurodevelopmental disorders[J]. Frontiers in molecular neuroscience, 2018, 11: 387.
[2] Palazzo E, Marabese I, Luongo L, et al. Nociception modulation by supraspinal group III metabotropic glutamate receptors[J]. Journal of Neurochemistry, 2017, 141(4): 507-519.
[3] Cristiano N, Cabayé A, Brabet I, et al. Novel inhibitory site revealed by XAP044 Mode of Action on the metabotropic glutamate 7 receptor Venus Flytrap Domain[J]. Journal of medicinal chemistry, 2024, 67(14): 11662-11687.
[4] Palazzo E, Romano R, Luongo L, et al. MMPIP, an mGluR7-selective negative allosteric modulator, alleviates pain and normalizes affective and cognitive behavior in neuropathic mice[J]. Pain, 2015, 156(6): 1060-1073.
[5] Gee C E, Peterlik D, Neuhäuser C, et al. Blocking metabotropic glutamate receptor subtype 7 (mGlu7) via the Venus flytrap domain (VFTD) inhibits amygdala plasticity, stress, and anxiety-related behavior[J]. Journal of Biological Chemistry, 2014, 289(16): 10975-10987.
[6] Estrela K A R, Senninger L, Arndt J, et al. Blocking metabotropic glutamate receptor subtype 7 via the Venus Flytrap Domain promotes a chronic stress-resilient phenotype in mice[J]. Cells, 2022, 11(11): 1817.
| Animal experiment [1]: | |
Animal models | Male CD1 mice |
Preparation Method | Adult male CD1 mice (20-25g) were housed under controlled illumination (12:12-hour light/dark cycle; light on 6 hours) and environmental conditions (room temperature: 20°C-22°C, humidity: 55%-60%) for at least 1 week before the beginning of experiments. Chow and tap water were available ad libitum. Mechanical allodynia was evaluated 14 days after spared nerve injury (SNI) or sham surgery by the dynamic plantar aesthesiometer. Mice were allowed to freely move in 1 of the 2 compartments of the enclosure, positioned on the metal mesh surface, and allowed to adapt to the testing environment before any measurement was taken. After 30-minute habituation period, the mechanical stimulus, a steel rod (2mm) pushed with ascending force (0-30g in 10 seconds), was delivered to the plantar surface of the hind paw of the mouse from below the floor of the test chamber by an automated testing device. When the mouse withdrew the hind paw, the mechanical stimulus was automatically stopped, and the force was recorded to the nearest 0.1g. Data were expressed as mechanical withdrawal threshold (MWT) and measured for 1 hour before and for 2 hours after a single vehicle (0.05% DMSO in saline), or XAP044 (30mg/kg; s.c.) administration. |
Dosage form | 30mg/kg for once; s.c. |
Applications | XAP044 treatment reversed mechanical allodynia in mice with SNI. |
References: | |
| Cas No. | 196928-50-4 | SDF | |
| Chemical Name | 7-hydroxy-3-(4-iodophenoxy)-4H-1-benzopyran-4-one | ||
| Canonical SMILES | O=C1C2=CC=C(O)C=C2OC=C1OC3=CC=C(I)C=C3 | ||
| Formula | C15H9IO4 | M.Wt | 380.1 |
| الذوبان | ≤10mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6309 mL | 13.1544 mL | 26.3089 mL |
| 5 mM | 526.2 μL | 2.6309 mL | 5.2618 mL |
| 10 mM | 263.1 μL | 1.3154 mL | 2.6309 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 1 reference(s) in Google Scholar.)