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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
109 Results for "
good bioavailability
" in MedChemExpress (MCE) Product Catalog:
Products (109)
109 Results for "good bioavailability" in MCE Product Catalog:
Cat. No.: HY-170961
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SDUY816 is an oral active dual APN/NEP inhibitor, with IC50 values of 0.68 μM for APN and 6.9 μM for NEP. SDUY816 exhibits analgesic effects and demonstrates good safety and pharmacokinetic profiles, with an oral bioavailability of 27% and a half-life of 4.02 hours in rats (oral administration, 10 mg/kg). SDUY816 has potential applications in the research of neuropathic pain disorders .
Cat. No.: HY-172768
CAS No.: 2930140-57-9
SCUT1-2 is a bifunctional antibacterial agent with good oral bioavailability in mice (F=56.8%). SCUT1-2 can kill the vegetative cells of C. difficile with a MIC of 0.06-0.50 μg/mL, and inhibit spore germination in vitro. SCUT1-2 could alleviate the symptoms of weight loss and diarrhea in mice caused by C. difficile infection (CDI) and prevent recurrent CDI .
Cat. No.: HY-177298
CAS No.: 366444-83-9
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PDE5-IN-15 (compound 21) is a xanthine derivative and PDE5 inhibitor, with IC50 values of 0.002, 0.180, 2.85 and 2.22 μM against hPDE5, bPDE6, bPDE1 and hPDE3, respectively. PDE5-IN-15 has good oral bioavailability in dogs. PDE5-IN-15 can be used in research on male erectile dysfunction .
Cat. No.: HY-162583
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PDE4-IN-17 (compound 4e) is a potent PDE4 inhibitor. PDE4-IN-17 inhibits PDE4B and PDE4D with IC50s of 10.0 and 15.2 nM, respectively. PDE4-IN-17 has good oral bioavailability (F=66%) and longer half-life (t1/2=2.0 h) in SD rats .
Cat. No.: HY-169986S
CAS No.: 2583719-08-6
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TyK2-IN-21-d3 (Compound 3c) is the orally active prodrug of the tyrosine kinase 2. TyK2-IN-21-d3 exhibits good chemical stability in aqueous system under different pHs. TyK2-IN-21-d3 alleviates the effect of gastric acid changes on drug absorption and improve the drug bioavailability in rat model .
Cat. No.: HY-171292
CAS No.: 3057263-82-5
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CK1δ-IN-9 (Compound 8) is the inhibitor for casein kinase 1 that inhibits CK1δ with IC50 of 1.4 nM. CK1δ-IN-9 inhibits p38α and p38β with IC50 of 0.25 μM and 0.78 μM. CK1δ-IN-9 exhibits pharmacokinetic characteristics with a good oral bioavailability (70%) and a moderate clearance .
Cat. No.: HY-175245
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hCA-IN-1 (Compound 5u) is an hCA inhibitor with Ki values of 159.2, 4.8, 15.5, and 2 nM against hCA I, hCA II, hCA IX, and hCA XII, respectively. hCA-IN-1 exhibits broad-spectrum anticancer activity against melanoma, breast, and colon cancer cells. ADME predictions indicate that hCA-IN-1 has good solubility and oral bioavailability. hCA-IN-1 can be used in tumor research .
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Antimicrobial agent-2 (compound V-a) is a broad-spectrum antimicrobial agent, possessing inhibitory activity against various Gram-positive and -negative bacteria. Antimicrobial agent-2 has excellent inhibitory effect on Methicillin-resistant Staphylococcus aureus (MRSA) with a MIC of 1 μg/mL. Antimicrobial agent-2 can effectively damage the membrane and lead to the leakage of protein, also can induce the generation of ROS. Antimicrobial agent-2 exhibits low toxicity, no obvious resistance and good bioavailability .
Cat. No.: HY-161940
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PCSK9-IN-30 (Compound 3f) is a PCSK9 inhibitor. PCSK9-IN-30 interacts with a cryptic binding groove of PCSK9, inhibiting the binding of PCSK9 to the low-density lipoprotein receptor (LDLR) (IC50 = 537 nM), restoring the uptake of low-density lipoprotein (LDL) by liver cells, and ultimately reducing plasma cholesterol levels. PCSK9-IN-30 exhibits good bioavailability in mice and can be used for research in the field of cardiovascular diseases .
Cat. No.: HY-122608
CAS No.: 1394808-82-2
Synonyms: SUVN-G3031 free base
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Samelisant (SUVN-G3031) free base is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant free base has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant free base can be used for the research of sleep-related disorders .
Cat. No.: HY-122058
CAS No.: 1097732-62-1
KRH-3955 is a CXCR4 antagonist with good bioavailability and potent anti-HIV-1 activity. KRH-3955 can effectively inhibit the replication of X4 HIV-1, including clinical isolates from different donors. KRH-3955 also shows activity against recombinant X4 HIV-1 containing reverse transcriptase, protease and tyrosinase resistance mutations. KRH-3955 can inhibit the binding of SDF-1alpha to CXCR4 and calcium ion signaling through this receptor. KRH-3955 inhibits the binding of an antibody against CXCR4 to CXCR4, showing a potent antagonistic effect on CXCR4. KRH-3955 shows an oral bioavailability of 25.6% in rats and can inhibit the replication of X4 HIV-1 in vivo .
Cat. No.: HY-112142A
CAS No.: 422547-55-5
Synonyms: DVR-23
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(Rac)-AB-423 (DVR-23) is an anti-HBV candidate compound with promising anti-HBV activity. (Rac)-AB-423 showed no induction of CYP1A2, CYP3A4, or CYP2B6 enzyme activity at high concentrations. (Rac)-AB-423 exhibited desirable pharmacokinetic properties, enabling good systemic exposure and high oral bioavailability. (Rac)-AB-423 achieved more than 2 log viral load reduction in the hydrodynamic injection (HDI) HBV mouse model .
Cat. No.: HY-118285
CAS No.: 579482-31-8
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Ro4491533 is a selective, negative allosteric mGluR2/3 receptor modulator that is equally effective on both subtypes. Ro4491533 can completely block glutamate-induced calcium mobilization and glutamate-induced [35S]GTPγS binding accumulation. Ro4491533 has good pharmacokinetic properties in mice and rats, high oral bioavailability, and can pass through the blood-brain barrier. Ro4491533 can also reverse the motor inhibition effect of LY379268 in mice and show antidepressant activity in the forced swim test and tail suspension test.
Cat. No.: HY-144122
CAS No.: 2757182-99-1
HIV-1 inhibitor-15 (compound 9d) is a highly potent and broad-spectrum HIV-1 inhibitor. HIV-1 inhibitor-15 has inhibitory activity against HIV-1 WT, L100I, K103N, Y181C, E138K with EC50s of 1.7 nM, 4 nM, 2 nM, 6 nM and 9 nM, respectively. HIV-1 inhibitor-15 has good solubility, safety profiles and favorable oral bioavailability .
Cat. No.: HY-170832
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Menin–KMT2A-IN-1 (Compound 20) is the inhibitor for menin–KMT2A that binds to menin with an IC50 of 8 nM, and inhibits the interaction between menin and lysine methyltransferase 2A (KMT2A). Menin–KMT2A-IN-1 inhibits hERG with an IC50 of 65 μM. Menin–KMT2A-IN-1 inhibits cell MV4-11 with an IC50 of 74 nM. Menin–KMT2A-IN-1 exhibits good pharmacokinetic characteristics in CD-1 mouse with an orally bioavailability of 74% .
Cat. No.: HY-173032
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VU6033685 is the orally active positive allosteric modulator (PAM) for mGlu1 that positively modulates human mGlu1 and human mGlu5 with EC50 of 39 nM and 3960 nM. VU6033685 also inhibits CYP1A2, CYP2C9 and CYP2D6 with IC50 of 26, 22.3 and 23.8 μM, respectively. VU6033685 reverses amphetamine-induced rats hyperlocomotion, protects rats from MK-801 (HY-15084B)-induced cognitive impairment. VU6033685 exhibits good pharmacokinetics characteristics in rats with an oral bioavailability of 42.8% .
Cat. No.: HY-176221
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α-Glucosidase-IN-92 (compound 14b) is a non-competitive inhibitor targeting α-glucosidase (IC50=64.0 μM), with better inhibitory potency than Acarbose (HY-B0089) (IC50=750 μM). α-Glucosidase-IN-92 has good oral bioavailability and can cross the blood-brain barrier. α-Glucosidase-IN-92 can delay carbohydrate hydrolysis and reduce postprandial blood glucose. α-Glucosidase-IN-92 can be used in anti-glycemic research for type 2 diabetes .
Cat. No.: HY-15007
CAS No.: 138382-23-7
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L 366509 is a spiroindenylpiperidine camphorsulfonamide oxytocin (OT) antagonist. Modifications led to a new series of o-tolylpiperazine (TP) camphorsulfonamides, exhibiting high affinity for OT receptors and selectivity over arginine vasopressin receptors. Notably, compound 7 (L-368,899) showed excellent OT receptor affinity, potency in inhibiting OT-stimulated uterine contractions, good aqueous solubility, and oral bioavailability in multiple species. Compound 7 has entered clinical testing as an oral and intravenous tocolytic agent. Molecular modeling suggests the TP camphorsulfonamide structure mimics the D-AA2-Ile3 dipeptide, crucial in potent OT antagonists .
Cat. No.: HY-N2345R
CAS No.: 23567-23-9
Category:
other families Flavonoids Phenols Polyphenols Plants Biflavones
Cat. No.: HY-169177
CAS No.: 3047795-60-5
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JNK-1-IN-4 (Compound E1) is an inhibitor for JNK, that inhibits JNK-1, JNK-2 and JNK-3 with IC50s of 2.7, 19.0 and 9.0 nM, respectively. JNK-1-IN-4 inhibits the phosphorylation of c-Jun, and reduces the expression of TGF-β1-induced EMT marker proteins, such as fibronectin and α-SMA. JNK-1-IN-4 exhibits good pharmacokinetic characteristics with a bioavailability of 69%. JNK-1-IN-4 exhibits anti-fibrotic effect in Bleomycin (HY-17565)-induced mice idiopathic pulmonary fibrosis models .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
