Search Result

Results for "

in vivo pharmacokinetic studies

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (2) Casein Kinase (1) CDK (1) Epigenetic Reader Domain (1) FLT3 (1) Fluorescent Dye (1) iGluR (1) Isotope-Labeled Compounds (1) Keap1-Nrf2 (1) Liposome (1) MAPKAPK2 (MK2) (1) NO Synthase (1) PD-1/PD-L1 (1) Prostaglandin Receptor (2) PROTACs (1) RXFP Receptor (1) SHP2 (1) VEGFR (1)
By Research Areas:	Cancer (7) Cardiovascular Disease (1) Endocrinology (2) Inflammation/Immunology (2) Neurological Disease (2)
Oligonucleotides:	Fluorescent Lipids (1) Pegylated Lipids (1)

Inhibitors & Agonists

Biochemical Assay Reagents

Peptides

Isotope-Labeled Compounds

Oligonucleotides

Targets Recommended: Dan family AIM2 CD44 NEKs

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-W440913

DSPE-PEG5000-Cy5	Liposome Fluorescent Dye	Cancer
DSPE-PEG-Cy5, MW 5000 is a fluorescently labeled PEGylated phospholipid with a molecular weight of 5000 Da. After intravenous injection, DSPE-PEG-Cy5, MW 5000 shows only extremely low fluorescence accumulation at tumor sites in orthotopic tumor-bearing mice, and can be used as a negative control for evaluating tumor accumulation of nanoparticles. DSPE-PEG-Cy5, MW 5000 can serve as a fluorescent marker to prepare Cy5-labeled NPs-DPPA and NPs-DPPA (C3F8) for pharmacokinetic and biodistribution studies in mice. DSPE-PEG-Cy5, MW 5000 is widely applicable to research in fields related to triple-negative breast cancer, hepatocellular carcinoma and so on .

HY-174424

NPH16	PD-1/PD-L1 Apoptosis	Cancer
NPH16 is an orally active PD-1/PD-L1 inhibitor with an IC₅₀ of 24.4 nM. NPH16 can promote HepG2 cell apoptosis. NPH16 shows excellent in vivo antitumor efficacy and favorable pharmacokinetic properties. NPH16 can be used for the study of liver cancer .

HY-145226

XY-06-007	PROTACs Epigenetic Reader Domain	Cancer
XY-06-007 is a selective and potent bump-and-hole (B&H)-PROTAC BRD4_BD1L94V degrader. XY-06-007 shows a DC_{50, 6 h} of 10 nM against BRD4_BD1L94V with no degradation of off-targets. XY-06-007 demonstrates suitable pharmacokinetics for in vivo studies .

HY-157928

Keap1-Nrf2-IN-18	Keap1-Nrf2	Inflammation/Immunology
Keap1-Nrf2-IN-18 (Compound 22) is an orally active Keap1-Nrf2 protein-protein interaction (PPI) inhibitor with good pharmacokinetics (PK) profiles and more potent in vivo activities in rats. Keap1-Nrf2-IN-18 has the strongest inhibitory activity in structure−activity relationship (SAR) study (K_D = 0.0029 μM) .

HY-136659

Ro 04-5595	iGluR	Others
Ro 04-5595 is a selective antagonist with specific activity against the NR2B subunit of the NMDA receptor. Ro 04-5595 exhibits favorable pharmacokinetic properties in in vitro and in vivo studies, with rapid uptake and clearance. Ro 04-5595 exhibits strong binding in NR2B receptor-enriched regions and low binding in the cerebellum. Ro 04-5595 is able to effectively inhibit specific binding, showing high affinity for the NR2B receptor and a clear ranking of binding affinity with a variety of other compounds .

HY-168715

SHP2-IN-33	SHP2 Apoptosis MAPKAPK2 (MK2)	Cancer
SHP2-IN-33 (Compound D13) is an allosteric inhibitor of SHP2 with an IC₅₀ of 1.2 μM. In cellular studies, SHP2-IN-33 demonstrates antiproliferative activity with an IC₅₀ of 38 μM against Huh7 cells by arresting the G0/G1 cell cycle, promoting apoptosis (Apoptosis), and suppressing the MAPK signaling pathway. In an in vivo Huh7 xenograft mouse model, SHP2-IN-33 exhibits significant antitumor activity and favorable pharmacokinetics, including 54% oral bioavailability and a half-life of 10.57 hours. SHP2-IN-33 is a promising compound for studying tumor diseases associated with SHP2 .

HY-13590

CEP-7055	VEGFR	Cancer
CEP-7055 (compound 21) is a novel vascular endothelial growth factor R2 (VEGF-R2) tyrosine kinase inhibitor with potent inhibitory activity. Studies have found that the inhibitor activity can be significantly improved by optimizing the R9 substituent. Compound 21 has potent low nanomolar inhibition of human VEGF-R tyrosine kinase and shows good selectivity against multiple tyrosine and serine/threonine kinases. N,N-dimethylglycine ester 40 was prepared to improve its water solubility and oral bioavailability. In animal pharmacokinetic studies, a significant increase in the plasma level of 21 was observed after oral administration of 40. Compound 21 showed significant in vivo antitumor activity in multiple tumor models and has entered phase I clinical trials as a water-soluble N,N-dimethylglycine ester proagent of 40 (CEP-7055).

HY-129934

Latanoprost ethyl amide Lat-NEt	Prostaglandin Receptor	Endocrinology
Latanoprost ethyl amide (Lat-NEt) is a latanoprost analog in which the C-1 carboxyl group has been modified to an N-ethyl amide. Prostaglandin esters have been shown to have ocular hypotensive activity.1 Prostaglandin N-ethyl amides were recently introduced as alternative prostaglandin ocular hypotensive prodrugs. Although it has been claimed that prostaglandin ethyl amides are not converted to the free acids in vivo, studies in our laboratories have shown that bovine and human corneal tissue converts the N-ethyl amides of various prostaglandins to the free acids with a conversion rate of about 2.5 μg/g corneal tissue/hr. Lat-NEt would be expected to show the typical intraocular effects of Latanoprost free acid, but with the much slower hydrolysis pharmacokinetics of the prostaglandin N-amides.

HY-129934S

Latanoprost ethyl amide-d4 Lat-NEt-d₄	Isotope-Labeled Compounds Prostaglandin Receptor	Endocrinology
Latanoprost ethyl amide-d₄ (Lat-NEt-d₄) is deuterium labeled Latanoprost ethyl amide. Latanoprost ethyl amide (Lat-NEt) is a latanoprost analog in which the C-1 carboxyl group has been modified to an N-ethyl amide. Prostaglandin esters have been shown to have ocular hypotensive activity.1 Prostaglandin N-ethyl amides were recently introduced as alternative prostaglandin ocular hypotensive prodrugs. Although it has been claimed that prostaglandin ethyl amides are not converted to the free acids in vivo, studies in our laboratories have shown that bovine and human corneal tissue converts the N-ethyl amides of various prostaglandins to the free acids with a conversion rate of about 2.5 μg/g corneal tissue/hr. Lat-NEt would be expected to show the typical intraocular effects of Latanoprost free acid, but with the much slower hydrolysis pharmacokinetics of the prostaglandin N-amides .

HY-P11625

R9-13	RXFP Receptor	Cardiovascular Disease
R9-13 is a fatty acid-conjugated relaxin and an agonist of LGR7 (RXFP1). R9-13 induces sustained pubic symphysis elongation in estrogen-pretreated mice. R9-13 exhibits long-acting pharmacokinetic profiles in rodents, with in vivo activity lasting up to one week after administration. R9-13 can be used in studies related to acute heart failure .

HY-181711

nNOS-IN-6	NO Synthase	Neurological Disease Cancer
nNOS-IN-6 is a human neuronal nitric oxide synthase (hnNOS) inhibitor with a human hnNOS K_i of 16 nM, ~1800-fold selectivity over human eNOS, ~2900-fold selectivity over human iNOS, and a rat nNOS K_i of 34 nM.nNOS-IN-6 exhibits high effective permeability in PAMPA-BBB assays, crosses the blood-brain barrier, and shows sustained systemic exposure, low clearance, and robust brain penetration in mouse in vivo pharmacokinetic studies.nNOS-IN-6 can be used for the research of neurodegenerative diseases, melanoma .

HY-123859

SR-2890	Casein Kinase FLT3 CDK	Neurological Disease Inflammation/Immunology Cancer
SR-2890 is a highly selective, ATP-competitive inhibitor of casein kinase CK1δ and CK1ε, with IC₅₀ values of 4 nM and 44 nM, respectively, and a K_i of 14 nM for CK1δ. SR-2890 exhibits antiproliferative effects. SR-2890 blocks the serine/threonine kinase activity of CK1δ and weakly inhibits a few off-target kinases such as FLT3, CDK4. SR-2890 has an oral bioavailability of 10% and a blood-brain barrier penetration rate of <1%. SR-2890 demonstrates stable in vitro metabolism and favorable in vivo pharmacokinetic properties, effectively inhibiting the growth of human A375 melanoma cells. SR-2890 can be used in melanoma research and is also a useful compound for studying CK1δ/ε-related diseases such as Alzheimer's disease .

Cat. No.	Product Name	Type

HY-W440913

DSPE-PEG5000-Cy5	Biochemical Assay Reagents
DSPE-PEG-Cy5, MW 5000 is a fluorescently labeled PEGylated phospholipid with a molecular weight of 5000 Da. After intravenous injection, DSPE-PEG-Cy5, MW 5000 shows only extremely low fluorescence accumulation at tumor sites in orthotopic tumor-bearing mice, and can be used as a negative control for evaluating tumor accumulation of nanoparticles. DSPE-PEG-Cy5, MW 5000 can serve as a fluorescent marker to prepare Cy5-labeled NPs-DPPA and NPs-DPPA (C3F8) for pharmacokinetic and biodistribution studies in mice. DSPE-PEG-Cy5, MW 5000 is widely applicable to research in fields related to triple-negative breast cancer, hepatocellular carcinoma and so on .

DSPE-PEG5000-Cy5

Biochemical Assay Reagents

DSPE-PEG-Cy5, MW 5000 is a fluorescently labeled PEGylated phospholipid with a molecular weight of 5000 Da. After intravenous injection, DSPE-PEG-Cy5, MW 5000 shows only extremely low fluorescence accumulation at tumor sites in orthotopic tumor-bearing mice, and can be used as a negative control for evaluating tumor accumulation of nanoparticles. DSPE-PEG-Cy5, MW 5000 can serve as a fluorescent marker to prepare Cy5-labeled NPs-DPPA and NPs-DPPA (C3F8) for pharmacokinetic and biodistribution studies in mice. DSPE-PEG-Cy5, MW 5000 is widely applicable to research in fields related to triple-negative breast cancer, hepatocellular carcinoma and so on .

Cat. No.	Product Name	Target	Research Area

HY-P11625

R9-13	RXFP Receptor	Cardiovascular Disease
R9-13 is a fatty acid-conjugated relaxin and an agonist of LGR7 (RXFP1). R9-13 induces sustained pubic symphysis elongation in estrogen-pretreated mice. R9-13 exhibits long-acting pharmacokinetic profiles in rodents, with in vivo activity lasting up to one week after administration. R9-13 can be used in studies related to acute heart failure .

Cat. No.	Product Name	Chemical Structure

HY-129934S

Latanoprost ethyl amide-d4
Latanoprost ethyl amide-d₄ (Lat-NEt-d₄) is deuterium labeled Latanoprost ethyl amide. Latanoprost ethyl amide (Lat-NEt) is a latanoprost analog in which the C-1 carboxyl group has been modified to an N-ethyl amide. Prostaglandin esters have been shown to have ocular hypotensive activity.1 Prostaglandin N-ethyl amides were recently introduced as alternative prostaglandin ocular hypotensive prodrugs. Although it has been claimed that prostaglandin ethyl amides are not converted to the free acids in vivo, studies in our laboratories have shown that bovine and human corneal tissue converts the N-ethyl amides of various prostaglandins to the free acids with a conversion rate of about 2.5 μg/g corneal tissue/hr. Lat-NEt would be expected to show the typical intraocular effects of Latanoprost free acid, but with the much slower hydrolysis pharmacokinetics of the prostaglandin N-amides .

Latanoprost ethyl amide-d4

Latanoprost ethyl amide-d₄ (Lat-NEt-d₄) is deuterium labeled Latanoprost ethyl amide. Latanoprost ethyl amide (Lat-NEt) is a latanoprost analog in which the C-1 carboxyl group has been modified to an N-ethyl amide. Prostaglandin esters have been shown to have ocular hypotensive activity.1 Prostaglandin N-ethyl amides were recently introduced as alternative prostaglandin ocular hypotensive prodrugs. Although it has been claimed that prostaglandin ethyl amides are not converted to the free acids in vivo, studies in our laboratories have shown that bovine and human corneal tissue converts the N-ethyl amides of various prostaglandins to the free acids with a conversion rate of about 2.5 μg/g corneal tissue/hr. Lat-NEt would be expected to show the typical intraocular effects of Latanoprost free acid, but with the much slower hydrolysis pharmacokinetics of the prostaglandin N-amides .

Cat. No.	Product Name		Classification

HY-W440913

DSPE-PEG5000-Cy5		Pegylated Lipids Fluorescent Lipids
DSPE-PEG-Cy5, MW 5000 is a fluorescently labeled PEGylated phospholipid with a molecular weight of 5000 Da. After intravenous injection, DSPE-PEG-Cy5, MW 5000 shows only extremely low fluorescence accumulation at tumor sites in orthotopic tumor-bearing mice, and can be used as a negative control for evaluating tumor accumulation of nanoparticles. DSPE-PEG-Cy5, MW 5000 can serve as a fluorescent marker to prepare Cy5-labeled NPs-DPPA and NPs-DPPA (C3F8) for pharmacokinetic and biodistribution studies in mice. DSPE-PEG-Cy5, MW 5000 is widely applicable to research in fields related to triple-negative breast cancer, hepatocellular carcinoma and so on .

Inquiry Online

Your information is safe with us. * Required Fields.

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社重松貿易株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Name
Email *

	Sorry, but the email address you supplied was invalid.