RO5328673
RO5328673 is an orally active, blood-brain barrier permeable neurokinin receptor antagonist that effectively targets human NK3 receptors (Ki=0.4 nM, Ka=0.1 nM), human NK2 receptors (Ki=1.1 nM, Ka=0.9 nM), and guinea pig NK3 receptors (Ka=0.1 nM and 0.13 nM). RO5328673 acts as an insurmountable antagonist of NK3 receptors with a slow dissociation rate, while it shows rapid association and dissociation rates at human NK2 receptors. RO5328673 potently inhibits senktide (HY-P0187)-induced enhancement of spontaneous activity in dopaminergic neurons and reverses senktide-induced changes in motor activity of gerbils. RO5328673 is widely applicable to research related to schizophrenia.
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- CAS No.: 1310817-94-7
- 화학식: C29H32Cl2FN3O4
- 분자량:576.49
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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
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
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hNK2 1.1 nM (Ki) |
hNK3 0.4 nM (Ki) |
In Vitro
RO5328673 (0.0003-10 μM) binds to hNK2 and hNK3 receptors with high affinity, with corresponding Ki values of 1.1 nM and 0.4 nM, respectively, while it shows weak affinity for the hNK1 receptor (Ki=52.8 nM)[1].
[3H]RO5328673 (0.01-20 nM; 23 °C for hNK2, hNK3, gpNK3 or 37 °C for gpNK3) binds with high affinity to a single saturable site on hNK2, hNK3 and gpNK3 receptors, and its binding to gpNK3 is temperature-independent[1].
RO5328673 (1-300 nM; 20 min) acts as an insurmountable antagonist of hNK3 and gpNK3 receptors, which reduces the maximal response intensity and potency of [MePhe7]NKB, with a stronger effect on gpNK3[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mongolian gerbils (male and female, weight 40-70 g)[1]
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Dosage:10 mg/kg; 30 mg/kg
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Administration:p.o.
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Result:Robustly reversed senktide-induced locomotor activity, with group mean total distance traveled reduced compared to vehicle-treated controls.
Produced plasma levels of 688 ng/mL (10 mg/kg dose) and 3508 ng/mL (30 mg/kg dose).
Produced brain levels of 360 ng/mL (10 mg/kg dose) and 1748 ng/mL (30 mg/kg dose).
Resulted in a brain/plasma ratio of 0.5 for both doses.
Chemical Information
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CAS No. 1310817-94-7
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분자량 576.49
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화학식 C29H32Cl2FN3O4
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SMILES
FC(C=C1)=CC=C1OC(N([C@H]2[C@H](C3=CC(Cl)=C(C=C3)Cl)CN(C2)C(C4CCN(CC4)C(C5(CC5)C)=O)=O)C)=O
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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.
Protocol
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Human pluripotent stem cell midbrain dopaminergic neuron differentiation
Human pluripotent stem cells are directed toward midbrain dopaminergic neurons by first inducing a neural floor-plate-like progenitor state, then patterning cells with ventralizing SHH signaling and midbrain/WNT-FGF cues, and finally maturing progenitors into neurons expressing dopaminergic markers such as TH, NURR1/NR4A2, PITX3, DAT/SLC6A3, VMAT2/SLC18A2, GIRK2/KCNJ6, FOXA2, LMX1A, and EN1. The main readouts are loss of pluripotency, acquisition of FOXA2+/LMX1A+ midbrain floor-plate progenitors, emergence of βIII-tubulin+/MAP2+ neurons, and production of TH+ dopaminergic neurons with molecular, dopamine-release, and electrophysiological features of midbrain dopaminergic identity.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
RO5328673 Related Classifications
HY-182423 Related Classifications
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