Atagabalin
Atagabalin (PD 0200390) is a Voltage-gated Calcium channel α2δ subunit binder with an IC50 of 22 nM. Atagabalin regulates neurotransmitter release by inhibiting calcium influx at high neuronal firing rates. Atagabalin can be used in research related to sleep disorders.
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- CAS No.: 223445-75-8
- 화학식: C10H19NO2
- 분자량:185.26
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
All Calcium Channel Isoforms
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Biological Activity
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Calcium Channel |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
10 μM
Compound: 5
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Inhibition of L-type amino acid transporter expressed in CHO cells assessed as inhibition of [3H]leucine uptake
Inhibition of L-type amino acid transporter expressed in CHO cells assessed as inhibition of [3H]leucine uptake
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[PMID: 20005103] |
Atagabalin potently binds to the VGCC α2δ subunit with an IC50 of 22 nM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 223445-75-8
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분자량 185.26
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화학식 C10H19NO2
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SMILES
O=C(O)CC1(CN)C[C@H](C)[C@@H](C)C1
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Synonyms
PD 0200390
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[1]. Kjellsson MC, et al. Modeling sleep data for a new drug in development using markov mixed-effects models. Pharmaceutical research. 2011 Oct;28(10):2610-27. [Content Brief]
[2]. Corrigan B, et al. Effect of renal impairment on the pharmacokinetics of PD 0200390, a novel ligand for the voltage-gated calcium channel alpha-2-delta subunit. British journal of clinical pharmacology. 2009 Aug;68(2):174-80. [Content Brief]
[3]. Chen Y, et al. Review of Voltage-gated Calcium Channel α2δ Subunit Ligands for the Treatment of Chronic Neuropathic Pain and Insight into Structure-activity Relationship (SAR) by Pharmacophore Modeling. Current medicinal chemistry. 2022 Aug 15;29(30):5097-5112. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Atagabalin Related Classifications
HY-14856 Related Classifications
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- Atagabalin
- 223445-75-8
- PD 0200390
- PD0200390
- PD-0200390
- Calcium Channel
- renal excretion
- neurotransmitter release
- calcium channel α2δ subunit
- insomnia
- sleep disturbance
- slow-wave sleep
- rapid eye movement sleep
- pharmacophore modeling
- voltage-gated calcium channel alpha-2-delta subunits
- calcium influx
- Inhibitor
- inhibitor
- inhibit